Free shipping on all orders over $ 500

GSK180736A

Cat. No. M5269
GSK180736A Structure
Synonym:

GSK180736

Size Price Availability Quantity
5mg USD 72  USD80 In stock
10mg USD 103.5  USD115 In stock
50mg USD 360  USD400 In stock
100mg USD 675  USD750 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

GSK180736A exhibits a 770 nM IC50 value against GRK2 and 300-fold less potency against GRK5. It is a weak inhibitor of PKA with an IC50 of 30 μM, but highly potent against ROCK1 (IC50 = 100 nM).

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 365.36
Formula C19H16FN5O2
CAS Number 817194-38-0
Purity >98%
Solubility 73 mg/mL in DMSO
Storage at -20°C
References

Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors.
Waldschmidt HV, et al. J Med Chem. 2016 Apr 28;59(8):3793-807. PMID: 27050625.

Crystal Structure of G Protein-coupled Receptor Kinase 5 in Complex with a Rationally Designed Inhibitor.
Homan KT, et al. J Biol Chem. 2015 Aug 21;290(34):20649-59. PMID: 26032411.

Identification and structure-function analysis of subfamily selective G protein-coupled receptor kinase inhibitors.
Homan KT, et al. ACS Chem Biol. 2015 Jan 16;10(1):310-9. PMID: 25238254.

Related ROCK Products
SAR407899

SAR407899 is a potent and selective, ATP-competitive ROCK inhibitor with IC50 of 135 nM for ROCK-2, and Kis of 36 nM and 41 nM for human and rat ROCK-2, respectively.

Belumosudil mesylate

Belumosudil mesylate (SLx-2119 mesylate) is an orally bioavailable inhibitor of ROCK-II that is greater than 200-fold selective over ROCK-I (IC50s = 105 nM and 24 µM, respectively).

BDP5290

BDP5290 is a potent inhibitor of both ROCK and MRCK with IC50s of 5 nM, 50 nM, 10 nM and 100 nM for ROCK1, ROCK2, MRCKα and MRCKβ, respectively.

Belumosudil (SLx-2119)

SLx-2119, also known as KD-025, is an orally bioavailable inhibitor of ROCK-II with IC50 of 105 nM.

ZINC00881524

ZINC00881524 is a potent and selective ROCK inhibitor.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GSK180736A, GSK180736 supplier, ROCK, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.