目录号 | 产品详情 | 靶点 | |
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TP1966 | |||
Cell-permeable peptide cleaved from protease-activated receptor 1 (PAR1) upon receptor activation. Attenuates endothelial cell migration and proliferation (IC50 ~ 20 μM), and induces cell cycle arrest. Promotes activation of caspase-3 and exhibits pro-apo | |||
T68499 | |||
F 15845 is a blocker of the persistent sodium current prevents consequences of hypoxia in rat femoral artery. F15845 has been shown to selectively inhibit the persistent sodium current of Nav1.5[1] exerting cardioprotective effects following ischemia. In vitro testing showed minimal effects of F15845 on other important ion channels of the heart, including major Ca2+ and K+ channels.[1] This characteristic is thought to account for the limited effect of F15845 to change other heart parameters such as basal cardiac function, hemodynamic functions and ventricular fibrillation. F15845 was also shown to exert improved effects when the membrane potential was depolarized,[1] by acting on the extracellular side of the channel. | |||
T71910 | |||
Racemic rasagiline,也称为 AGN-1135,是一种单胺氧化酶 B 型抑制剂(MAOI)。然而,在食用富含酪胺的食物的患者中,这种药物的应用可能导致致命的高血压危象。TVP-1022是雷沙吉兰的(S)异构体,具有心脏保护剂的作用。 | |||
T60713 | |||
TK-129 是具有口服活性的 KDM5B 的有效抑制剂,IC50值为44 nM,并且具有低毒性。TK-129 发挥心脏保护作用,通过抑制 KDM5B 和阻断 KDM5B 相关的 Wnt 通路。TK-129 可用于研究心血管疾病,它能在体内减少异丙肾上腺素诱导的心肌重塑和纤维化,并且在体外减少 Ang II 诱导的心脏成纤维细胞活化。 | |||
T35494 | |||
(±)11(12)-EET is a fully racemic version of the R/S enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes.[1][2][3[]A higher proportion of 11(R),12(S)-EET is produced by the CYP450 isoforms CYP2C23 and CYP2C24 while CYP2B2 produces a higher proportion of 11(S),12(R)-EET.[3]11(12)-EET has been shown, along with 8(9)-EET to play a role in the recovery of depleted calcium pools in cultured smooth muscle cells[4] It also inhibits basolateral 18-pS potassium channels in the renal cortical collecting duct when used at a concentration of 100 nM.[5]11(12)-EET (50 μg/kg per day) increases adhesion of isolated peripheral blood leukocytes in a chamber coated with P-selectin and ICAM-1 but does not affect choroidal neovascularization size following laser photocoagulation[6] It also has anti-inflammatory, angiogenic, and cardioprotective properties[7] | |||
T37496 | |||
Alamandine can be formed from angiotensin A by action of ACE-2 or directly from angiotensin-(1-7) by decarboxylation of its aspartate residue. The angiotensin A analog produces effects resembling those of Ang II (1-7). However, it acts independently of the two known vasodilators receptors of the RAS (Mas and angiotensin II type 2). To produce its effects, alamandine binds to the Mas-related receptor, MrgD. A novel orally active formulation of alamandine produced a long-term antihypertensive effect in spontaneously hypertensive rats and cardioprotective effects. These novel findings will be helpful for developing a new understanding of the RAS, a key regulator of blood pressure and fluid balance. The heptapeptide could serve as a model peptide, e.g. in the development and evaluation of analytical methods. | |||
T37495 | |||
Angiotensin 1-7 (Ang-(1-7)) acetate 是RAS中的一种内源性七肽,具备心脏保护作用,主要表现为对心肌细胞的抗炎与抗纤维化活性。该化合物能抑制纯化的犬ACE活性(IC50=0.65 μM),通过降低ACE活性并促进一氧化氮释放,作为血管舒张调节的局部协同因子。此外,Angiotensin 1-7 acetate 可阻止血管紧张素Ⅱ诱发的平滑肌细胞增殖和肥大,同时对内皮细胞表现出抗血管生成和生长抑制作用。 | |||
T36482 | |||
Water-soluble salt of lamotrigine . Displays anticonvulsant effects and inhibits glutamate release, possibly through inhibition of Na+, K+ and Ca2+ currents. Leach et al (1991) Neurochemical and behavioral aspects of lamotr. Epilepsia 32 S4 PMID:1685439 |Smith and Meldrum (1995) Cardioprotective effect of lamotr. after focal ischemia in rats. Stroke 26 117 PMID:7839380 |Zona and Avoli (1997) Lamotrigine reduces voltage-gated sodium currents in rat central neurons in culture. Epilepsia 38 522 PMID:9184596 |Grunze et al (1998) Modulation of calcium and potassium currents by lamotr. Neuropsychobiology 38 131 PMID:9778600 | |||
T36722 | |||
Deltorphin II is a peptide agonist of δ2-opioid receptors.1,2It is selective for δ-opioid receptors over μ- and κ-opioid receptors in radioligand bindings assays (Kis = 0.0033, >1, and >1 μM, respectively) and induces [35S]GTPγS binding in mouse brain membrane preparations (EC50= 0.034 μM). Deltorphin II (0.12 mg/kg) decreases the infarction zone:risk zone ratio in a rat model of myocardial ischemia-reperfusion injury induced by coronary occlusion, an effect that can be reversed by the δ2-opioid receptor antagonist naltriben but not the δ1-opioid receptor antagonist BNTX.3Intrathecal administration of deltorphin II (15 μg/animal) increases latency to withdraw in the paw pressure and tail-flick tests in rats.4 1.Raynor, K., Kong, H., Chen, Y., et al.Pharmacological characterization of the cloned κ-, δ-, and μ-opioid receptorsMol. Pharm.45(2)330-334(1994) 2.Scherrer, G., Befort, K., Contet, C., et al.The delta agonists DPDPE and deltorphin II recruit predominantly mu receptors to produce thermal analgesia: A parallel study of mu, delta and combinatorial opioid receptor knockout miceEur. J. Neurosci.19(8)2239-2248(2004) 3.Maslov, L.N., Barzakh, E.I., Krylatov, A.V., et al.Opioid peptide deltorphin II simulates the cardioprotective effect of ischemic preconditioning: role of δ2-opioid receptors, protein kinase C, and KATP channelsBull. Exp. Biol. Med.149(5)591-593(2010) 4.Labuz, D., Toth, G., Machelska, H., et al.Antinociceptive effects of isoleucine derivatives of deltorphin I and deltorphin II in rat spinal cord: A search for selectivity of delta receptor subtypesNeuropeptides32(6)511-517(1998) |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPJ-00734 | KNG1 Protein, Human, Recombinant (His) | Human | Human Cells | ||
Kininogen-1 is a secreted protein which contains three cystatin domains. There are two alternatively spliced forms, designated as the high molecular weight (HMW) and low MW (LMW) forms. Kininogen-1 plays a critical role in blood coagulation and inflammatory response. Kininogens are inhibitors of thiol proteases. Kininogen-1 participates in blood coagulation by helping to position optimally prekallikrein and factor XI next to factor XII, also inhibits the thrombin- and plasmin-induced aggregation of thrombocytes. The active peptide bradykinin that is released from Kininogen-1 shows a variety of physiological effects: influence in smooth muscle contraction, induction of hypotension, natriuresis and diuresis, decrease in blood glucose level. It is a mediator of inflammation and causes increase in vascular permeability, stimulation of nociceptors release of other mediators of inflammation. It has a cardioprotective effect. LMW-kininogen inhibits the aggregation of thrombocytes and doesn’t involved in blood clotting.
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TMPY-01606 | Kininogen 1 Protein, Mouse, Recombinant (His) | Mouse | HEK293 | ||
Kininogen-1, also known as high molecular weight kininogen, Williams-Fitzgerald-Flaujeac factor, Alpha-2-thiol proteinase inhibitor, Fitzgerald factor, KNG1, and BDK, is a secreted protein that contains three cystatin domains. Kininogen-1 / KNG1 is a protein from the blood coagulation system as well as the kinin-kallikrein system. It is a protein that adsorbs to the surface of biomaterials that come in contact with blood. Kininogen-1 / KNG1 circulates throughout the blood and quickly adsorbs to the material surfaces. Kininogen-1 / KNG1 is one of the early participants of the intrinsic pathway of coagulation, together with Factor XII (Hageman factor) and prekallikrein. Kininogen-1 / KNG1 is one of the kininogens, a class of proteins. As with many other coagulation proteins, the protein was initially named after the patients in whom deficiency was first observed. When the clinical data were combined, it turned out that all patients had a deficiency of the same protein. Defects in KNG1 are the cause of high molecular weight kininogen deficiency (HMWK deficiency) which is an autosomal recessive coagulation defect. Patients with HWMK deficiency do not have a hemorrhagic tendency, but they exhibit abnormal surface-mediated activation of fibrinolysis.
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TMPY-01598 | Kininogen 1 Protein, Human, Recombinant (His) | Human | HEK293 | ||
Kininogen-1, also known as high molecular weight kininogen, Williams-Fitzgerald-Flaujeac factor, Alpha-2-thiol proteinase inhibitor, Fitzgerald factor, KNG1, and BDK, is a secreted protein that contains three cystatin domains. Kininogen-1 / KNG1 is a protein from the blood coagulation system as well as the kinin-kallikrein system. It is a protein that adsorbs to the surface of biomaterials that come in contact with blood. Kininogen-1 / KNG1 circulates throughout the blood and quickly adsorbs to the material surfaces. Kininogen-1 / KNG1 is one of the early participants of the intrinsic pathway of coagulation, together with Factor XII (Hageman factor) and prekallikrein. Kininogen-1 / KNG1 is one of the kininogens, a class of proteins. As with many other coagulation proteins, the protein was initially named after the patients in whom deficiency was first observed. When the clinical data were combined, it turned out that all patients had a deficiency of the same protein. Defects in KNG1 are the cause of high molecular weight kininogen deficiency (HMWK deficiency) which is an autosomal recessive coagulation defect. Patients with HWMK deficiency do not have a hemorrhagic tendency, but they exhibit abnormal surface-mediated activation of fibrinolysis.
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