GSK269962 HCl
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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.


Price and Availability

Size
Price

50mg
USD 450
500mg
USD 2650
5g
USD 8450
Size
Price

100mg
USD 850
1g
USD 3450
Size
Price

200mg
USD 1530
2g
USD 5250

GSK269962 HCl, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

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


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


Technical Data

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).

Harmonized System Code:
2934990300


References

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.