A TRPV4 agonist
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GSK1016790A

Item No. 17289

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(1S)-1-[[4-[(2S)-2-[[(2,4-dichlorophenyl)sulfonyl]amino]-3-hydroxy-1-oxopropyl]-1-piperazinyl]carbonyl]-3-methylbutyl]-benzo[b]thiophene-2-carboxamide
CAS Number
942206-85-1
Synonyms
  • GSK101
Molecular Formula
C28H32Cl2N4O6S2
Formula Weight
655.6
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 15 mg/mlDMSO: 15 mg/mlDMSO:PBS(pH 7.2) (1:3): 0.25 mg/mlEthanol: 10 mg/ml
λmax
223, 231, 286 nm
SMILES
ClC1=CC=C(S(N[C@H](C(N2CCN(C([C@@H](NC(C3=CC4=C(C=CC=C4)S3)=O)CC(C)C)=O)CC2)=O)CO)(=O)=O)C(Cl)=C1
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $95

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    10 mg

    $153

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    25 mg

    $294

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    Product Description

    Transient receptor potential vanilloid 4 (TRPV4) is a nonselective cation channel thought to be involved in osmoregulation, hyperalgesia, and control of epithelial cell volume. GSK1016790A is a TRPV4 agonist that has been reported to elicit calcium influx in HEK cells expressing mouse or human TRPV4 (EC50s = 18 and 2.1 nM, respectively).1 It has been used to demonstrate a role for TRPV4 in regulating urinary bladder activity and endothelial control of vascular tone.1,2,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Thorneloe, K.S., Sulpizio, A.C., Lin, Z., et al. 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. 326(2), 432-442 (2008).

    2. Willette, R.N., Bao, W., Nerurkar, S., et al. Systemic activation of the transient receptor potential vanilloid subtype 4 channel causes endothelial failure and circulatory collapse: Part 2. J. Pharmacol. Exp. Ther. 326(2), 443-452 (2008).

    3. Adapala, R.K., Talasila, P.K., Bratz, I.N., et al. PKCα mediates acetylcholine-induced activation of TRPV4-dependent calcium influx in endothelial cells. Am. J. Physiol. Heart Circ. Physiol. 301(3), H757-H765 (2011).