GSK269962 HCl
new
featured

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 555430

CAS#: 2095432-71-4 (HCl)

Description: GSK269962 is a selective ROCK inhibitor with IC50 values of 1.6 and 6 nM for ROCK-I and ROCK-II, respectively. GSK 269962 could reverse corticosterone-induced depressive-like behaviour and changes in cystometric parameters associated with detrusor overactivity, as well as undo the alterations of several biomarkers related to both disorders (i.e., pro-inflammatory/anti-inflammatory cytokines and neurotrophins) in serum, urinary bladder, and different brain structures.


Chemical Structure

img
GSK269962 HCl
CAS# 2095432-71-4 (HCl)

Theoretical Analysis

MedKoo Cat#: 555430
Name: GSK269962 HCl
CAS#: 2095432-71-4 (HCl)
Chemical Formula: C29H31ClN8O5
Exact Mass: 0.00
Molecular Weight: 607.068
Elemental Analysis: C, 57.38; H, 5.15; Cl, 5.84; N, 18.46; O, 13.18

Price and Availability

Size Price Availability Quantity
50mg USD 450 2 weeks
100mg USD 850 2 weeks
200mg USD 1530 2 weeks
500mg USD 2650 2 weeks
1g USD 3450 2 weeks
Bulk inquiry

Related CAS #: 925213-80-5 (3HCl)   850664-21-0 (free base)   2095432-71-4 (HCl)    

Synonym: GSK269962 HCl; GSK269962 hydrochloride; GSK269962; GSK 269962; GSK-269962; GSK269962A; GSK 269962A; GSK-269962A; GSK26996B;

IUPAC/Chemical Name: N-[3-[[2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-1H-imidazo[4,5-c]pyridin-6-yl]oxy]phenyl]-4-[2-(4-morpholinyl)ethoxy]-benzamide hydrochloride

InChi Key: UYKVMFKKKLLDGL-UHFFFAOYSA-N

InChi Code: InChI=1S/C29H30N8O5.ClH/c1-2-37-24-17-25(31-18-23(24)33-28(37)26-27(30)35-42-34-26)41-22-5-3-4-20(16-22)32-29(38)19-6-8-21(9-7-19)40-15-12-36-10-13-39-14-11-36;/h3-9,16-18H,2,10-15H2,1H3,(H2,30,35)(H,32,38);1H

SMILES Code: O=C(NC1=CC=CC(OC2=CC3=C(N=C(C4=NON=C4N)N3CC)C=N2)=C1)C5=CC=C(OCCN6CCOCC6)C=C5.[H]Cl

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Biological target: GSK269962A hydrochloride (GSK 269962 hydrochloride) is a potent ROCK inhibitor with IC50s of 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively.
In vitro activity: In this article, this study characterized two aminofurazan-based inhibitors, GSK269962A [N-(3-{[2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-1H-imidazo[4, 5-c]pyridin-6-yl]oxy}phenyl)-4-{[2-(4-morpholinyl)ethyl]-oxy}benzamide] and SB-7720770-B [4-(7-{[(3S)-3-amino-1-pyrrolidinyl]carbonyl}-1-ethyl-1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-amine], as members of a novel class of compounds that potently inhibit ROCK enzymatic activity. GSK269962A and SB-772077-B have IC50 values of 1.6 and 5.6 nM toward recombinant human ROCK1, respectively. GSK269962A also exhibited more than 30-fold selectivity against a panel of serine/threonine kinases. Reference: J Pharmacol Exp Ther. 2007 Jan;320(1):89-98. https://pubmed.ncbi.nlm.nih.gov/17018693/
In vivo activity: CYP injection resulted in a significant increase in cystometric parameters: basal pressure, threshold pressure, bladder contraction duration, relaxation time, detrusor overactivity index, non-voiding contractions amplitude, and non-voiding contractions frequency as well as increased Evans Blue extravasation into bladder tissue, whereas micturition voiding pressure, voided volume, post-void residual, volume threshold, intercontraction interval, bladder compliance, and volume threshold to elicit non-voiding contractions as well as urothelium thickness were significantly decreased in CYP-injected rats. Administration of GSK 269962 normalized the abovementioned CYP injection-induced changes. Inhibition of ROCK was found to ameliorate CYP-induced detrusor overactivity and bladder inflammation. Reference: Naunyn Schmiedebergs Arch Pharmacol. 2017 Jun;390(6):613-619. https://pubmed.ncbi.nlm.nih.gov/28220212/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 100.0 164.73
Ethanol 28.0 46.12

Preparing Stock Solutions

The following data is based on the product molecular weight 607.07 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Doe C, Bentley R, Behm DJ, Lafferty R, Stavenger R, Jung D, Bamford M, Panchal T, Grygielko E, Wright LL, Smith GK, Chen Z, Webb C, Khandekar S, Yi T, Kirkpatrick R, Dul E, Jolivette L, Marino JP Jr, Willette R, Lee D, Hu E. Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. J Pharmacol Exp Ther. 2007 Jan;320(1):89-98. doi: 10.1124/jpet.106.110635. Epub 2006 Oct 3. PMID: 17018693. 2. Wróbel A, Doboszewska U, Rechberger E, Rojek K, Serefko A, Poleszak E, Skalicka-Woźniak K, Dudka J, Wlaź P. Rho kinase inhibition ameliorates cyclophosphamide-induced cystitis in rats. Naunyn Schmiedebergs Arch Pharmacol. 2017 Jun;390(6):613-619. doi: 10.1007/s00210-017-1361-8. Epub 2017 Feb 21. PMID: 28220212; PMCID: PMC5411406.
In vitro protocol: 1. Doe C, Bentley R, Behm DJ, Lafferty R, Stavenger R, Jung D, Bamford M, Panchal T, Grygielko E, Wright LL, Smith GK, Chen Z, Webb C, Khandekar S, Yi T, Kirkpatrick R, Dul E, Jolivette L, Marino JP Jr, Willette R, Lee D, Hu E. Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities. J Pharmacol Exp Ther. 2007 Jan;320(1):89-98. doi: 10.1124/jpet.106.110635. Epub 2006 Oct 3. PMID: 17018693.
In vivo protocol: 1. Wróbel A, Doboszewska U, Rechberger E, Rojek K, Serefko A, Poleszak E, Skalicka-Woźniak K, Dudka J, Wlaź P. Rho kinase inhibition ameliorates cyclophosphamide-induced cystitis in rats. Naunyn Schmiedebergs Arch Pharmacol. 2017 Jun;390(6):613-619. doi: 10.1007/s00210-017-1361-8. Epub 2017 Feb 21. PMID: 28220212; PMCID: PMC5411406.

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

1: Wróbel A, Serefko A, Rechberger E, Banczerowska-Górska M, Poleszak E, Dudka J, Skorupska K, Miotła P, Semczuk A, Kulik-Rechberger B, Mandziuk S, Rechberger T. Inhibition of Rho kinase by GSK 269962 reverses both corticosterone-induced detrusor overactivity and depression-like behaviour in rats. Eur J Pharmacol. 2018 Oct 15;837:127-136. doi: 10.1016/j.ejphar.2018.08.027. Epub 2018 Aug 30. PubMed PMID: 30172788.

2: Wróbel A, Doboszewska U, Rechberger E, Rojek K, Serefko A, Poleszak E, Skalicka-Woźniak K, Dudka J, Wlaź P. Rho kinase inhibition ameliorates cyclophosphamide-induced cystitis in rats. Naunyn Schmiedebergs Arch Pharmacol. 2017 Jun;390(6):613-619. doi: 10.1007/s00210-017-1361-8. Epub 2017 Feb 21. PubMed PMID: 28220212; PubMed Central PMCID: PMC5411406.

3: Wróbel A, Rechberger T. The Influence of Maxacalcitol, Vitamin D3 Analog, on Detrusor Overactivity in Conscious Rats. Urology. 2016 Jul;93:224.e7-224.e15. doi: 10.1016/j.urology.2016.03.008. Epub 2016 Mar 23. PubMed PMID: 27018369.

4: Wróbel A, Rechberger T. Ovariectomy May Induce Detrusor Overactivity in Rats: The Therapeutic Role of Rho Kinase Inhibition. Urology. 2016 Jul;93:225.e1-7. doi: 10.1016/j.urology.2016.03.007. Epub 2016 Mar 14. PubMed PMID: 26988893.

5: Wróbel A, Rechberger T. The effect of combined treatment with a β(3) AR agonist and a ROCK inhibitor on detrusor overactivity. Neurourol Urodyn. 2017 Mar;36(3):580-588. doi: 10.1002/nau.22978. Epub 2016 Feb 16. PubMed PMID: 26879338.

6: Wróbel A, Rechberger T. The influence of Rho-kinase inhibition on acetic acid-induced detrusor overactivity. Neurourol Urodyn. 2017 Feb;36(2):263-270. doi: 10.1002/nau.22918. Epub 2015 Nov 6. PubMed PMID: 26546786.

7: Hutchinson JL, Rajagopal SP, Yuan M, Norman JE. Lipopolysaccharide promotes contraction of uterine myocytes via activation of Rho/ROCK signaling pathways. FASEB J. 2014 Jan;28(1):94-105. doi: 10.1096/fj.13-237040. Epub 2013 Sep 27. PubMed PMID: 24076962.