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GSK-180736A
CAS No. 817194-38-0
GSK-180736A( GSK 180736A | GSK180736A )
Catalog No. M16042 CAS No. 817194-38-0
A highly selective and potent GRK2 inhibitor with IC50 of 0.77 uM.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 43 | In Stock |
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| 5MG | 60 | In Stock |
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| 10MG | 81 | In Stock |
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| 50MG | 291 | In Stock |
|
| 100MG | 538 | In Stock |
|
| 200MG | Get Quote | In Stock |
|
| 500MG | Get Quote | In Stock |
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| 1G | Get Quote | In Stock |
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Biological Information
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Product NameGSK-180736A
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NoteResearch use only, not for human use.
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Brief DescriptionA highly selective and potent GRK2 inhibitor with IC50 of 0.77 uM.
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DescriptionA highly selective and potent GRK2 inhibitor with IC50 of 0.77 uM; displays >400-fold selective for GRK2 over both GRK1 and GRK5, with no inhibition on PKA; also inhibits ROCK with IC50 of 0.1 uM.
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In VitroGSK180736A is a compound structurally similar to paroxetine that is developed as a ROCK inhibitor, is shown to be an even more potent and selective inhibitor of GRK2 with an IC50 of 0.77 μM and more than 100-fold selectivity over other GRKs. ROCK1 is a potential therapeutic target in the treatment of cardiovascular diseases such as hypertension. GSK180736A is a weak inhibitor of PKA with an IC50 of 30 μM, but highly potent against ROCK1 (IC50=100 nM).
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In Vivo——
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SynonymsGSK 180736A | GSK180736A
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PathwayOthers
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TargetGRK (GPCRK)
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RecptorGRK1|GRK2|GRK5|PKA|ROCK
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Research Area——
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Indication——
Chemical Information
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CAS Number817194-38-0
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Formula Weight365.3611
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Molecular FormulaC19H16FN5O2
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Purity>98% (HPLC)
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SolubilityDMSO: ≥ 30 mg/mL
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SMILESCC1=C(C(NC(=O)N1)C2=CC=C(C=C2)F)C(=O)NC3=CC4=C(C=C3)NN=C4
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Chemical Name5-Pyrimidinecarboxamide, 4-(4-fluorophenyl)-1,2,3,4-tetrahydro-N-1H-indazol-5-yl-6-methyl-2-oxo-
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Homan KT, et al. ACS Chem Biol. 2015 Jan 16;10(1):310-9.
2. Waldschmidt HV, et al. J Med Chem. 2016 Apr 28;59(8):3793-807.
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