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MedKoo Cat#: 527099 | Name: GSK360A
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Description:

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

GSK360A, also known as GSK 1120360A, is a novel inhibitor of prolyl hydroxylase (PHD) domain-containing enzyme.

Chemical Structure

GSK360A
GSK360A
CAS#931399-19-8

Theoretical Analysis

MedKoo Cat#: 527099

Name: GSK360A

CAS#: 931399-19-8

Chemical Formula: C17H17FN2O5

Exact Mass: 348.1121

Molecular Weight: 348.33

Elemental Analysis: C, 58.62; H, 4.92; F, 5.45; N, 8.04; O, 22.97

Price and Availability

Size Price Availability Quantity
5mg USD 350.00 Back order
25mg USD 1,250.00 Back order
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Related CAS #
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Synonym
GSK360A; GSK 360A; GSK-360A; GSK 1120360A; GSK1120360A; GSK-1120360A;
IUPAC/Chemical Name
{[1-(2-Cyclopropyl-ethyl)-6-fluoro-4-hydroxy-2-oxo-1,2-dihydro-quinoline-3-carbonyl]-amino}-acetic acid
InChi Key
TYHRZQVUPPODPT-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H17FN2O5/c18-10-3-4-12-11(7-10)15(23)14(16(24)19-8-13(21)22)17(25)20(12)6-5-9-1-2-9/h3-4,7,9,23H,1-2,5-6,8H2,(H,19,24)(H,21,22)
SMILES Code
O=C(O)CNC(C1=C(O)C2=C(N(CCC3CC3)C1=O)C=CC(F)=C2)=O
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
>2 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
Product Data
Instruction
View handling instruction
Biological target:
GSK360A, also known as GSK 1120360A, is a novel inhibitor of prolyl hydroxylase (PHD) domain-containing enzyme.
In vitro activity:
Likewise, post-OGD (oxygen-glucose deprivation) treatment with 3 or 30 μM GSK360A caused greater survival of OL (oligodendrocytes) (Fig. 3C, p-value by one-way ANOVA, 3 independent cultures for each group) and a dose-dependent increase of Ho1, Epo, Vegf, Glut1 mRNAs at 24 h (Fig. 3D, n > 3 independent cultures for each group). These results support cytoprotective effects of GSK360A-mediated HIF1α-stabilization against OGD. Reference: Neurobiol Dis. 2021 Jan;148:105200. https://pubmed.ncbi.nlm.nih.gov/33248237/
In vivo activity:
The oral administration of GSK360A significantly upregulated HIF-1α target EPO and VEGF levels in rat plasma (Fig 4). Rats treated with GSK360A exhibited a significantly decreased overall number of shocks compared to vehicle group (e.g., group factor p<0.0001). Reference: PLoS One. 2017 Sep 7;12(9):e0184049. https://pubmed.ncbi.nlm.nih.gov/28880966/

Preparing Stock Solutions

The following data is based on the product molecular weight 348.33 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. Kuan CY, Chen HR, Gao N, Kuo YM, Chen CW, Yang D, Kinkaid MM, Hu E, Sun YY. Brain-targeted hypoxia-inducible factor stabilization reduces neonatal hypoxic-ischemic brain injury. Neurobiol Dis. 2021 Jan;148:105200. doi: 10.1016/j.nbd.2020.105200. Epub 2020 Nov 26. PMID: 33248237. 2. Zhou J, Li J, Rosenbaum DM, Zhuang J, Poon C, Qin P, Rivera K, Lepore J, Willette RN, Hu E, Barone FC. The prolyl 4-hydroxylase inhibitor GSK360A decreases post-stroke brain injury and sensory, motor, and cognitive behavioral deficits. PLoS One. 2017 Sep 7;12(9):e0184049. doi: 10.1371/journal.pone.0184049. PMID: 28880966; PMCID: PMC5589177. 3. Gumucio JP, Flood MD, Bedi A, Kramer HF, Russell AJ, Mendias CL. Inhibition of prolyl 4-hydroxylase decreases muscle fibrosis following chronic rotator cuff tear. Bone Joint Res. 2017 Jan;6(1):57-65. doi: 10.1302/2046-3758.61.BJR-2016-0232.R1. PMID: 28108482; PMCID: PMC5301902.
In vitro protocol:
1. Kuan CY, Chen HR, Gao N, Kuo YM, Chen CW, Yang D, Kinkaid MM, Hu E, Sun YY. Brain-targeted hypoxia-inducible factor stabilization reduces neonatal hypoxic-ischemic brain injury. Neurobiol Dis. 2021 Jan;148:105200. doi: 10.1016/j.nbd.2020.105200. Epub 2020 Nov 26. PMID: 33248237.
In vivo protocol:
1. Zhou J, Li J, Rosenbaum DM, Zhuang J, Poon C, Qin P, Rivera K, Lepore J, Willette RN, Hu E, Barone FC. The prolyl 4-hydroxylase inhibitor GSK360A decreases post-stroke brain injury and sensory, motor, and cognitive behavioral deficits. PLoS One. 2017 Sep 7;12(9):e0184049. doi: 10.1371/journal.pone.0184049. PMID: 28880966; PMCID: PMC5589177. 2. Gumucio JP, Flood MD, Bedi A, Kramer HF, Russell AJ, Mendias CL. Inhibition of prolyl 4-hydroxylase decreases muscle fibrosis following chronic rotator cuff tear. Bone Joint Res. 2017 Jan;6(1):57-65. doi: 10.1302/2046-3758.61.BJR-2016-0232.R1. PMID: 28108482; PMCID: PMC5301902.
1: Zhou J, Li J, Rosenbaum DM, Zhuang J, Poon C, Qin P, Rivera K, Lepore J, Willette RN, Hu E, Barone FC. The prolyl 4-hydroxylase inhibitor GSK360A decreases post-stroke brain injury and sensory, motor, and cognitive behavioral deficits. PLoS One. 2017 Sep 7;12(9):e0184049. doi: 10.1371/journal.pone.0184049. eCollection 2017. PubMed PMID: 28880966; PubMed Central PMCID: PMC5589177. 2: Ong SG, Lee WH, Theodorou L, Kodo K, Lim SY, Shukla DH, Briston T, Kiriakidis S, Ashcroft M, Davidson SM, Maxwell PH, Yellon DM, Hausenloy DJ. HIF-1 reduces ischaemia-reperfusion injury in the heart by targeting the mitochondrial permeability transition pore. Cardiovasc Res. 2014 Oct 1;104(1):24-36. doi: 10.1093/cvr/cvu172. Epub 2014 Jul 25. PubMed PMID: 25063991. 3: Sen Banerjee S, Thirunavukkarasu M, Tipu Rishi M, Sanchez JA, Maulik N, Maulik G. HIF-prolyl hydroxylases and cardiovascular diseases. Toxicol Mech Methods. 2012 Jun;22(5):347-58. doi: 10.3109/15376516.2012.673088. Review. PubMed PMID: 22424133. 4: Beuck S, Schänzer W, Thevis M. Hypoxia-inducible factor stabilizers and other small-molecule erythropoiesis-stimulating agents in current and preventive doping analysis. Drug Test Anal. 2012 Nov;4(11):830-45. doi: 10.1002/dta.390. Epub 2012 Feb 24. Review. PubMed PMID: 22362605. 5: Bao W, Qin P, Needle S, Erickson-Miller CL, Duffy KJ, Ariazi JL, Zhao S, Olzinski AR, Behm DJ, Pipes GC, Jucker BM, Hu E, Lepore JJ, Willette RN. Chronic inhibition of hypoxia-inducible factor prolyl 4-hydroxylase improves ventricular performance, remodeling, and vascularity after myocardial infarction in the rat. J Cardiovasc Pharmacol. 2010 Aug;56(2):147-55. doi: 10.1097/FJC.0b013e3181e2bfef. PubMed PMID: 20714241.