GSK1016790A
GSK1016790A, also known as GSK101, is a TRPV4 agonist that elicits calcium influx in HEK cells expressing mouse or human TRPV4 (EC50s = 18 and 2.1 nM, respectively).
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化学信息
| 名称 | GSK1016790A |
|---|---|
| Iupac 化学名称 | N-[(2S)-1-[4-[(2S)-2-[(2,4-dichlorophenyl)sulfonylamino]-3-hydroxypropanoyl]piperazin-1-yl]-4-methyl-1-oxopentan-2-yl]-1-benzothiophene-2-carboxamide |
| 同义词 | GSK1016790A; GSK-1016790A; GSK 1016790A; GSK101; GSK-101; GSK 101; |
| 英文同义词 | GSK1016790A; GSK-1016790A; GSK 1016790A; GSK101; GSK-101; GSK 101; |
| 分子式 | C28H32Cl2N4O6S2 |
| 分子量 | 655.61 |
| Smile | O=C(C1=CC2=CC=CC=C2S1)N[C@@H](CC(C)C)C(N3CCN(C([C@@H](NS(=O)(C4=CC=C(Cl)C=C4Cl)=O)CO)=O)CC3)=O |
| InChiKey | IVYQPSHHYIAUFO-VXKWHMMOSA-N |
| InChi | InChI=1S/C28H32Cl2N4O6S2/c1-17(2)13-21(31-26(36)24-14-18-5-3-4-6-23(18)41-24)27(37)33-9-11-34(12-10-33)28(38)22(16-35)32-42(39,40)25-8-7-19(29)15-20(25)30/h3-8,14-15,17,21-22,32,35H,9-13,16H2,1-2H3,(H,31,36)/t21-,22-/m0/s1 |
| Cas号 | 942206-85-1 |
| 相关CAS号 |
订购信息
| 包装 | 价格 | 库存 | 纯度 | 备货期 |
|---|---|---|---|---|
| 大货 | 询价 | 询价 | 询价 |
| 外观性状 | 固体粉末 |
|---|---|
| 纯度 | 98% Min. |
| 存储 | 短期（几天到几周）为0-4摄氏度，长期（几个月）为-20摄氏度 |
| 可溶性 | 可溶于DMSO |
| 处理方式 | |
| 运输条件 | 作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周 |
| 海关编码 |
| Targets | |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Addison MP, Singh TU, Parida S, Choudhury S, Kasa JK, Sukumaran SV, Darzi SA, Kandasamy K, Singh V, Kumar D, Mishra SK. NO synthase inhibition attenuates EDHF-mediated relaxation induced by TRPV4 channel agonist GSK1016790A in the rat pulmonary artery: Role of TxA2. Pharmacol Rep. 2016 Jun;68(3):620-6. doi: 10.1016/j.pharep.2016.01.003. PubMed PMID: 26991376.
2: Pankey EA, Zsombok A, Lasker GF, Kadowitz PJ. Analysis of responses to the TRPV4 agonist GSK1016790A in the pulmonary vascular bed of the intact-chest rat. Am J Physiol Heart Circ Physiol. 2014 Jan 1;306(1):H33-40. doi: 10.1152/ajpheart.00303.2013. PubMed PMID: 24186096; PubMed Central PMCID: PMC3920159.
3: Sullivan MN, Francis M, Pitts NL, Taylor MS, Earley S. Optical recording reveals novel properties of GSK1016790A-induced vanilloid transient receptor potential channel TRPV4 activity in primary human endothelial cells. Mol Pharmacol. 2012 Sep;82(3):464-72. doi: 10.1124/mol.112.078584. PubMed PMID: 22689561; PubMed Central PMCID: PMC3422704.
4: Jin M, Wu Z, Chen L, Jaimes J, Collins D, Walters ET, O'Neil RG. Determinants of TRPV4 activity following selective activation by small molecule agonist GSK1016790A. PLoS One. 2011 Feb 14;6(2):e16713. doi: 10.1371/journal.pone.0016713. PubMed PMID: 21339821; PubMed Central PMCID: PMC3038856.
5: Thorneloe KS, Sulpizio AC, Lin Z, Figueroa DJ, Clouse AK, McCafferty GP, Chendrimada TP, Lashinger ES, Gordon E, Evans L, Misajet BA, Demarini DJ, Nation JH, Casillas LN, Marquis RW, Votta BJ, Sheardown SA, Xu X, Brooks DP, Laping NJ, Westfall TD. N-((1S)-1-{[4-((2S)-2-{[(2,4-dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1 -piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide (GSK1016790A), a novel and potent transient receptor potential vanilloid 4 channel agonist induces urinary bladder contraction and hyperactivity: Part I. J Pharmacol Exp Ther. 2008 Aug;326(2):432-42. doi: 10.1124/jpet.108.139295. Erratum in: J Pharmacol Exp Ther. 2011 Jul;338(1):410. PubMed PMID: 18499743.
