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Alternative_name
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; 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; TRPV4 channel agonist; Transient Receptor Potential Vanilloid 4 Channel Agonist
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Description
GSK1016790A is a transient receptor potential vanilloid 4 (TRPV4) agonist that elicits calcium influx in HEK cells expressing mouse or human transient TRPV4 with EC₅₀ values of 18 and 2.1 nM, respectively. It regulates urinary bladder activity and infusion of GSK1016790A into the bladders of TRPV4+/+ mice induces bladder overactivity.
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CAS Number
942206-85-1
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Structure Available
True
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Salt Form
false
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Molecular Formula
C₂₈H₃₂Cl₂N₄O₆S₂
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Molecular Weight
655.61
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Cell Permeable
True
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Purity
98%
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Solubilities
~10 mg/ml in in DMSO
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Handling
Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.
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Tag Line
An agonist of TRPV4
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Storage Condition
-20ºC
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Shipping Condition
RT
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Shelf Life
36months
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PubChem CID
23630211
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SMILES
CC(C)CC(C(=O)N1CCN(CC1)C(=O)C(CO)NS(=O)(=O)C2=C(C=C(C=C2)Cl)Cl)NC(=O)C3=CC4=CC=CC=C4S3
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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
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InChi Key
IVYQPSHHYIAUFO-VXKWHMMOSA-N
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MSDS Available
True
