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Merck
모든 사진(1)

문서

G0798

Sigma-Aldrich

GSK1016790A

≥98% (HPLC), solid, TRPV4 channel agonist

동의어(들):

GSK101, (N-((1S)-1-{[4-((2S)-2-{[(2,4-Dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide

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모든 사진(1)

About This Item

실험식(Hill 표기법):
C28H32Cl2N4O6S2
CAS Number:
942206-85-1
Molecular Weight:
655.61
MDL number:
MFCD12912413
UNSPSC 코드:
12352200
PubChem Substance ID:
329799716
NACRES:
NA.77

product name

GSK1016790A, ≥98% (HPLC)

분석

≥98% (HPLC)

형태

solid

색상

white

solubility

DMSO: >10 mg/mL

주관자

GlaxoSmithKline

저장 온도

−20°C

SMILES string

CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N3CCN(CC3)C(=O)[C@H](CO)NS(=O)(=O)c4ccc(Cl)cc4Cl

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

InChI key

IVYQPSHHYIAUFO-VXKWHMMOSA-N

애플리케이션

GSK1016790A has been used:
  • to stimulate transient receptor potential vanilloid 4 (TRPV4)-mediated currents in Xenopus laevis oocytes
  • to stimulate cells in Ca2+ level measurement in human retinal capillary endothelial cells (HRCECs)
  • to study the role of TRPV4 channels in brain injury after intracerebral hemorrhage (ICH)
  • to trigger the opening of TRPV4 channels in bovine nucleus pulposus cells or Hanks′ Balanced Salt Solution

생화학적/생리학적 작용

GSK1016790A is a novel and potent TRPV4 channel agonist. The TRPV4 (transient receptor potential vanilloid 4) member of the TRP superfamily has been implicated in numerous physiological processes. GSK1016790A elicited Ca2+ influx in mouse and human TRPV4 expressing HEK cells (EC50 values of 18 and 2.1 nM, respectively), and evoked a dose-dependent activation of TRPV4 whole-cell currents at concentrations above 1 nM. It is 300 fold more potent than 4a-PDD (Cat. No. P8014).

특징 및 장점

This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Storage Class Code

11 - Combustible Solids

WGK

WGK 1

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable

시험 성적서(COA)

제품의 로트/배치 번호를 입력하여 시험 성적서(COA)을 검색하십시오. 로트 및 배치 번호는 제품 라벨에 있는 ‘로트’ 또는 ‘배치’라는 용어 뒤에서 찾을 수 있습니다.

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문서 라이브러리 방문

When size matters: transient receptor potential vanilloid 4 channel as a volume-sensor rather than an osmo-sensor
Toft-Bertelsen TL, et al.
The Journal of Physiology, 595(11), 3287-3302 (2017)
TRPV4 channels stimulate Ca2+-induced Ca2+ release in mouse neurons and trigger endoplasmic reticulum stress after intracerebral hemorrhage
Shen J, et al.
Brain Research Bulletin, 146, 143-152 (2019)
TRPV4 regulates migration and tube formation of human retinal capillary endothelial cells
Wen L, et al.
BMC Ophthalmology, 18(1), 38-38 (2018)
Sandip M Swain et al.
The Journal of biological chemistry, 296, 100171-100171 (2020-12-11)
The ion channels Piezo1 and TRPV4 have both, independently, been implicated in high venous pressure- and fluid shear stress-induced vascular hyperpermeability in endothelial cells. However, the mechanism by which Piezo1 and TRPV4 channels execute the same function is poorly understood.
Reduced tissue osmolarity increases TRPV4 expression and pro-inflammatory cytokines in intervertebral disc cells
Walter BA, et al.
European Cells & Materials, 32, 123-123 (2016)
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문서

Transient Receptor Potential Channels

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