WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 522675
CAS#: 223387-75-5
Description: FG-2216, also known as YM311, is orally bioavailable HIF-prolyl hydroxylase inhibitor. FG-2216 induced significant and reversible Epo induction in vivo. FG-2216 showed the ability to stabilize HIF-α, to stimulate EPO secretion in in vitro studies, and to increase hematocrit, red blood cell count, and hemoglobin levels in an animal efficacy study.
MedKoo Cat#: 522675
Name: FG-2216
CAS#: 223387-75-5
Chemical Formula: C12H9ClN2O4
Exact Mass: 280.0251
Molecular Weight: 280.664
Elemental Analysis: C, 51.35; H, 3.23; Cl, 12.63; N, 9.98; O, 22.80
Synonym: FG-2216; FG 2216; FG2216; YM311; YM-311; YM 311.
IUPAC/Chemical Name: (1-chloro-4-hydroxyisoquinoline-3-carbonyl)glycine
InChi Key: OUQVKRKGTAUJQA-UHFFFAOYSA-N
InChi Code: InChI=1S/C12H9ClN2O4/c13-11-7-4-2-1-3-6(7)10(18)9(15-11)12(19)14-5-8(16)17/h1-4,18H,5H2,(H,14,19)(H,16,17)
SMILES Code: OC1=C(C(NCC(O)=O)=O)N=C(Cl)C2=CC=CC=C21
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, not in water
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
The following data is based on the product molecular weight 280.664 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.
| 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 |
1: Hong YR, Kim HT, Lee SC, Ro S, Cho JM, Kim IS, Jung YH. [(4-Hydroxyl-benzo[4,5]thieno[3,2-c]pyridine-3-carbonyl)-amino]-acetic acid derivatives; HIF prolyl 4-hydroxylase inhibitors as oral erythropoietin secretagogues. Bioorg Med Chem Lett. 2013 Nov 1;23(21):5953-7. doi: 10.1016/j.bmcl.2013.08.067. Epub 2013 Aug 23. PubMed PMID: 24042008.
2: 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.
3: Beuck S, Bornatsch W, Lagojda A, Schänzer W, Thevis M. Development of liquid chromatography-tandem mass spectrometry-based analytical assays for the determination of HIF stabilizers in preventive doping research. Drug Test Anal. 2011 Nov-Dec;3(11-12):756-70. doi: 10.1002/dta.365. PubMed PMID: 22213684.
4: Bernhardt WM, Wiesener MS, Scigalla P, Chou J, Schmieder RE, Günzler V, Eckardt KU. Inhibition of prolyl hydroxylases increases erythropoietin production in ESRD. J Am Soc Nephrol. 2010 Dec;21(12):2151-6. doi: 10.1681/ASN.2010010116. Epub 2010 Nov 29. PubMed PMID: 21115615; PubMed Central PMCID: PMC3014028.
5: Beuck S, Schwabe T, Grimme S, Schlörer N, Kamber M, Schänzer W, Thevis M. Unusual mass spectrometric dissociation pathway of protonated isoquinoline-3-carboxamides due to multiple reversible water adduct formation in the gas phase. J Am Soc Mass Spectrom. 2009 Nov;20(11):2034-48. doi: 10.1016/j.jasms.2009.07.016. Epub 2009 Aug 7. PubMed PMID: 19734057.
6: Cases A. The latest advances in kidney diseases and related disorders. Drug News Perspect. 2007 Dec;20(10):647-54. PubMed PMID: 18301799.
7: Thevis M, Kohler M, Schlörer N, Schänzer W. Gas phase reaction of substituted isoquinolines to carboxylic acids in ion trap and triple quadrupole mass spectrometers after electrospray ionization and collision-induced dissociation. J Am Soc Mass Spectrom. 2008 Jan;19(1):151-8. Epub 2007 Nov 9. PubMed PMID: 18063383.
8: Hsieh MM, Linde NS, Wynter A, Metzger M, Wong C, Langsetmo I, Lin A, Smith R, Rodgers GP, Donahue RE, Klaus SJ, Tisdale JF. HIF prolyl hydroxylase inhibition results in endogenous erythropoietin induction, erythrocytosis, and modest fetal hemoglobin expression in rhesus macaques. Blood. 2007 Sep 15;110(6):2140-7. Epub 2007 Jun 8. PubMed PMID: 17557894; PubMed Central PMCID: PMC1976368.
