目录号 | 产品详情 | 靶点 | |
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T70575 | Others | ||
AS 183 is an inhibitor of cholesterol acyltransferase (ACAT). | |||
T9975 | Others | ||
GPR183 (3-(3,4-difluorophenyl)-N-[3-fluoro-5-(morpholin-4-yl)phenyl]propanamide) 是一种趋化受体,在 B 细胞中具有成熟作用,其内源性配体是氧甾醇 7α,25-二羟基胆固醇 (7α,25-OHC)。 GPR183 可用于炎症性肠病 (IBD) 的研究。 | |||
T37794 | Others | ||
Rec 15/2615 is an antagonist of α1B-adrenergic receptors (α1B-ARs; Ki = 0.45 nM for the recombinant human receptor).1 It selectively inhibits α1B-ARs over α1A-, α1D-, and α1L-ARs (Kis = 7.59, 10.23, and 49 nM, respectively). Rec 15/2615 inhibits norepinephrine-induced contractions of isolated rabbit prostate and urethral strips (Kis = 100 and 316.2 nM, respectively), as well as reduces norepinephrine-induced contractions of chloroethylclonidine-precontracted isolated rabbit aortic rings (Ki = 50 nM).2 It decreases diastolic blood pressure (ED25 = 183 μg/kg, i.v.) and increases intracavernous pressure in anesthetized dogs when administered intracavernously at doses ranging from 30 and 1,000 μg/kg.1,2 |1. Sironi, G., Colombo, D., Poggesi, E., et al. Effects of intracavernous administration of selective antagonists of α1-adrenoceptor subtypes on erection in anesthetized rats and dogs. J. Pharmacol. Exp. Ther. 292(3), 974-981 (2000).|2. Testa, R., Guarneri, L., Angelico, P., et al. Pharmacological characterization of the uroselective alpha-1 antagonist Rec 15/2739 (SB 216469): Role of the alpha-1L adrenoceptor in tissue selectivity, part II. J. Pharmacol. Exp. Ther. 281(3), 1284-1293 (1997). | |||
T36999 | Others | ||
Novel oxylipins, referred to as docosanoids, have been derived from C22polyunsaturated fatty acids 7(S),17(S)-dihydroxy-8(E),10(Z),13(Z),15(E),19(Z)-Docosapentaenoic acid (7(S),17(S)-hydroxy DPA) is a DPA-derived analog of the 17(S)-dihydroxy series of docosanoids known as protectins. Protectin D1, a DHA-derived dihydroxy fatty acid, exhibits potent anti-inflammatory activities.1,2,3Potentially, 7(S),17(S)-hydroxy DPA demonstrates similar properties; however, its biological activity has yet to be determined. 1.Serhan, C.N., Gotlinger, K., Hong, S., et al.Anti-inflammatory actions of neuroprotectin D1/protectin D1 and its natural stereoisomers: Assignments of dihydroxy-containing docosatrienesJ. Immunol.176(3)1848-1859(2006) 2.Ariel, A., and Serhan, C.N.Resolvins and protectins in the termination program of acute inflammationTRENDS in Immunology28(4)176-183(2007) 3.Schwab, J.M., Chiang, N., Arita, M., et al.Resolvin E1 and protectin D1 activate inflammation-resolution programmesNature447(7146)869-874(2007) | |||
T35836 | Others | ||
PMX-205 is a cyclic hexapeptide that acts as a potent antagonist of C5a receptor (C5aR; IC50= 31 nM).1It is orally active and blocks inflammatory signaling and symptoms in animal models of colitis and allergic asthma.2,3PMX-205 is also brain penetrant and reduces neuroinflammation and neurodegeneration in an animal model of Alzheimer's disease.4 1.March, D.R., Proctor, L.M., Stoermer, M.J., et al.Potent cyclic antagonists of the complement C5a receptor on human polymorphonuclear leukocytes. Relationships between structures and activityMol. Pharmacol.65(4)868-879(2004) 2.Jain, U., Woodruff, T.M., and Stadnyk, A.W.The C5a receptor antagonist PMX205 ameliorates experimentally induced colitis associated with increased IL-4 and IL-10Br. J. Pharmacol.168(2)488-501(2013) 3.Staab, E.B., Sanderson, S.D., Wells, S.M., et al.Treatment with the C5a receptor/CD88 antagonist PMX205 reduces inflammation in a murine model of allergic asthmaInt. Immunopharmacol.21(2)293-300(2014) 4.Fonseca, M.I., Ager, R.R., Chu, S.-H., et al.Treatment with a C5aR antagonist decreases pathology and enhances behavioral performance in murine models of Alzheimer's diseaseJ. Immunol.183(2)1375-1383(2009) | |||
T36779 | Others | ||
NG 25 is a type II kinase inhibitor that inhibits MAP4K2 and TAK1 (IC50s = 21.7 and 149 nM, respectively).1It also inhibits the Src family kinases Src and LYN (IC50s = 113 and 12.9 nM, respectively) and Abl family kinases (IC50s = 75.2 nM), as well as CSK, FER, and p38α (IC50s = 56.4, 82.3, and 102 nM, respectively). NG 25 (100 nM) prevents TNF-α-induced IKKα/β phosphorylation and IκB-α degradation in L929 cells. It inhibits secretion of IFN-α and IFN-β induced by CpG type B and CL097, respectively, in Gen2.2 cells in a concentration-dependent manner.2NG 25 decreases cell viability of HCT116KRASWT, and to a greater degree of HCT116KRASG13D, colorectal cancer cells in a concentration-dependent manner.3It also reduces tumor growth and increases the number of TUNEL-positive tumor cells in a CT26KRASG12Dmouse orthotopic model of colorectal cancer. 1.Tan, L., Nomanbhoy, T., Gurbani, D., et al.Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2)J. Med. Chem.58(1)183-196(2015) 2.Pauls, E., Shpiro, N., Peggie, M., et al.Essential role for IKKβ in production of type 1 interferons by plasmacytoid dendritic cellsJ. Biol. Chem. 287(23)19216-19228(2012) 3.Ma, Q., Gu, L., Liao, S., et al.NG25, a novel inhibitor of TAK1, suppresses KRAS-mutant colorectal cancer growth in vitro and in vivoApoptosis24(1-2)83-94(2019) | |||
T35527 | Others | ||
PI3Kα-IN-4 is a potent, selective and orally active inhibitor of PI3Kα, with an IC50 of 1.8 nM. PI3Kα-IN-4 has antitumor activity[1]. PI3Kα-IN-4 (compound 10) inhibits PI3Kα, β, δ, and γ, with IC50s of 1.8, 271.0, 13.9, and 13.8 nM, respectively in kinase assays[1].PI3Kα-IN-4 inhibits PI3Kα, β, δ, and γ, with IC50s of 12.1,1393, 183, and >10000 nM, respectively in cell based assays[1]. PI3Kα-IN-4 (compound 10) (30 mg/kg; p.o. once daily for 21 d) achieves the best efficacy, which could inhibit tumor growth by 73.0% in mice[1].PI3Kα-IN-4 (15-40 mg/kg; p.o. once daily for 30 d) dose dependently suppresses tumor growth by 62.5% (15 mg/kg), 86.0% (30 mg/kg) and 90.7% (40 mg/kg), respectively in mice[1].PI3Kα-IN-4 (15-40 mg/kg; p.o. once daily; 1-4 h) inhibits the phosphorylation of Akt in a dose- and time-dependent manner in vivo[1].PI3Kα-IN-4 shows high Cmax (mouse 22167, rat 2327 nM) and good bioavailability (mouse 59.4%, rat 46.9%) following oral administration (mouse 10, rat 3 mg/kg)[1].PI3Kα-IN-4 shows t1/2 (mouse 0.99, rat 1.22 h) and low plasma clearance (mouse 4.16, rat 5.28 mL/min/kg) following intravenous injection (mouse 1, rat 1 mg/kg)[1]. [1]. Dong J, et, al. Discovery of 3-Quinazolin-4(3 H)-on-3-yl-2, N-dimethylpropanamides as Orally Active and Selective PI3Kα Inhibitors. ACS Med Chem Lett. 2020 Jun 10; 11(7): 1463-1469. |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-01656 | VEGF183 Protein, Human, Recombinant | Human | Baculovirus Insect Cells | ||
VEGF183 Protein, Human, Recombinant is expressed in Baculovirus insect cells. The predicted molecular weight is 21 kDa and the accession number is P15692-3.
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TMPY-05798 | VEGF145 Protein, Human, Recombinant | Human | HEK293 Cells | ||
VEGF145 Protein, Human, Recombinant is expressed in HEK293 mammalian cells. The predicted molecular weight is 16.92 kDa and the accession number is P15692-6.
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TMPY-03080 | VEGF165 Protein, Danio rerio (zebrafish), Recombinant | Danio rerio (zebrafish) | Baculovirus Insect Cells | ||
VEGF165 Protein, Danio rerio (zebrafish), Recombinant is expressed in Baculovirus insect cells. The predicted molecular weight is 19.2 kDa and the accession number is O73682.
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TMPJ-00864 | VEGF165 Protein, Human, Recombinant | Human | HEK293 Cells | ||
Human Vascular endothelial growth factor (VEGF), also known as VEGF-A and vascular permeability factor (VPF), belongs to the platelet-derived growth factor family of cysteine-knot growth factors. It is a potent activator in vasculogenesis and angiogenesis both physiologically and pathologically. VEGF-A has 8 differently spliced isoforms, of which VEGF165 is the most abundant one. VEGF165 is a disulfide-linked homodimer consisting of two glycosylated 165 amino acid polypeptide chains. VEGF stimulates the cellular response through binding to tyrosine kinase receptors VEGFR1 and VEGFR2 on the cell surface. It is widely accepted that VEGFR2 mediate almost all of the known cellular responses to VEGF while the function of VEGFR1 is less defined and is thought to modulate the VEGFR2 signaling.
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TMPK-00822 | VEGF165 Protein, Human, Recombinant (His & Avi), FITC-Labeled | Human | HEK293 Cells | ||
Vascular endothelial growth factor (VEGF or VEGF-A), also known as vascular permeability factor (VPF), is a potent mediator of both angiogenesis and vasculogenesis in the fetus and adult. VEGF165 appears to be the most abundant and potent isoform, followed by VEGF121 and VEGF189. VEGF165 Protein, Human, Recombinant (His & Avi), FITC-Labeled is expressed in HEK293 mammalian cells with C-His-Avi tag. The predicted molecular weight is 22.2 kDa and the accession number is P15692-4.
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TMPY-03698 | VEGF121b Protein, Human, Recombinant | Human | HEK293 Cells | ||
VEGF121b Protein, Human, Recombinant is expressed in HEK293 mammalian cells. The predicted molecular weight is 34.10 kDa and the accession number is P15692-9.
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TMPY-03705 | VEGF164 Protein, Canine, Recombinant | Canine | HEK293 Cells | ||
VEGF164 Protein, Canine, Recombinant is expressed in HEK293 mammalian cells. The predicted molecular weight is 17 kDa and the accession number is Q9MYV3-3.
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TMPK-00826 | VEGF121 Protein, Human, Recombinant (His & Avi), Biotinylated | Human | HEK293 Cells | ||
Vascular endothelial growth factor (VEGF or VEGF-A), also known as vascular permeability factor (VPF), is a potent mediator of both angiogenesis and vasculogenesis in the fetus and adult. VEGF165 appears to be the most abundant and potent isoform, followed by VEGF121 and VEGF189. VEGF121 Protein, Human, Recombinant (His & Avi), Biotinylated is expressed in HEK293 mammalian cells with C-His-Avi tag. The predicted molecular weight is 17 kDa and the accession number is P15692-9.
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TMPY-02432 | VEGF164 Protein, Rat, Recombinant | Rat | Baculovirus Insect Cells | ||
VEGF164 Protein, Rat, Recombinant is expressed in Baculovirus insect cells. The predicted molecular weight is 19.2 kDa and the accession number is P16612-2.
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TMPY-04911 | VEGF165 Protein, Human, Recombinant (His & Avi), Biotinylated | Human,Cynomolgus | HEK293 Cells | ||
VEGF165 Protein, Human, Recombinant (His & Avi), Biotinylated is expressed in HEK293 mammalian cells with His and Avi tag. The predicted molecular weight is 23.1 kDa and the accession number is P15692-4.
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TMPJ-00865 | VEGF121 Protein, Human, Recombinant (His) | Human | HEK293 Cells | ||
Human VEGF121, also known as Vascular endothelial growth factor A, VEGFA, Vascular permeability factor, VPF and VEGF, is a homodimeric, heparin-binding glycoprotein which belongs to the platelet-derived growth factor (PDGF)/vascular endothelial growth factor (VEGF) family. VEGF-A is a glycosylated mitogen that specifically acts on endothelial cells and has various effects, including mediating increased vascular permeability, inducing angiogenesis, vasculogenesis, permeabilization of blood vessels and endothelial cell growth, increasing microvascular permeability, promoting cell migration and inhibiting apoptosis. Alternatively spliced transcript variants of VEGF-A encod either secreted or cell-associated isoforms. The lymphangiogenesis may be promoted by upregulation of VEGF121, which may in turn act in part via induction of VEGF-C. It binds to the FLT1/VEGFR1 and KDR/VEGFR2 receptors, heparan sulfate and heparin. NRP1/Neuropilin-1 binds isoforms VEGF-165 and VEGF-145. Isoform VEGF165B binds to KDR but does not activate downstream signaling pathways, does not activate angiogenesis and inhibits tumor growth.
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TMPY-01717 | VEGF164 Protein, Mouse, Recombinant | Mouse | Baculovirus Insect Cells | ||
VEGF164 Protein, Mouse, Recombinant is expressed in Baculovirus insect cells. The predicted molecular weight is 19.4 kDa and the accession number is Q00731-2.
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TMPK-00825 | VEGF121 Protein, Human, Recombinant (His & Avi) | Human | HEK293 Cells | ||
Vascular endothelial growth factor (VEGF or VEGF-A), also known as vascular permeability factor (VPF), is a potent mediator of both angiogenesis and vasculogenesis in the fetus and adult. VEGF165 appears to be the most abundant and potent isoform, followed by VEGF121 and VEGF189. VEGF121 Protein, Human, Recombinant (His & Avi) is expressed in HEK293 mammalian cells with C-His-Avi tag. The predicted molecular weight is 17 kDa and the accession number is P15692-9.
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