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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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M413917-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $117.90 | |
M413917-25mg | 25mg | In stock | $531.90 | |
M413917-100mg | 100mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $543.90 |
HIF Modulators
Synonyms | 3H-Pyrazol-3-one, 1,2-dihydro-2-[6-(4-morpholinyl)-4-pyrimidinyl]-4-(1H-1,2,3-triazol-1-yl)- | Molidustat(BAY 85-3934) | NCGC00388364-04 | UNII-9JH486CZ13 | 2-(6-Morpholin-4-Ylpyrimidin-4-Yl)-4-(1,2,3-Triazol-1-Yl)-1~{h}-Pyrazol-3-One | BCP14477 | DTXSID8 |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | Molidustat (BAY 85-3934) is a potent hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor with IC50 of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD, respectively. Phase 2. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Egl nine homolog 3 inhibitor |
Product Description | Information Molidustat (BAY 85-3934) Molidustat (BAY 85-3934) is a potent hypoxia-inducible factor prolyl hydroxylase ( HIF-PH ) inhibitor with IC50 of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD, respectively. Phase 2. Targets PHD2 (Cell-free assay); PHD3 (Cell-free assay); PHD1 (Cell-free assay) 280 nM; 450 nM; 480 nM In vitro Molidustat induces the transcription of hypoxia-sensitive genes in HeLa, A549, and Hep3B cells. In vivo In healthy Wistar rats and cynomolgus monkeys, Molidustat (1.5 mg/kg, p.o.) induces dose-dependent production of EPO and erythropoiesis. In rats with gentamicin-induced renal anemiabe, Molidustat (5 mg/kg, p.o.) is also effective in raising hematocrit levels while stimulating endogenous EPO production without hypertensive effects. |
ALogP | -0.2 |
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IUPAC Name | 2-(6-morpholin-4-ylpyrimidin-4-yl)-4-(triazol-1-yl)-1H-pyrazol-3-one |
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INCHI | InChI=1S/C13H14N8O2/c22-13-10(20-2-1-16-18-20)8-17-21(13)12-7-11(14-9-15-12)19-3-5-23-6-4-19/h1-2,7-9,17H,3-6H2 |
InChi Key | IJMBOKOTALXLKS-UHFFFAOYSA-N |
Canonical SMILES | C1COCCN1C2=NC=NC(=C2)N3C(=O)C(=CN3)N4C=CN=N4 |
Isomeric SMILES | C1COCCN1C2=NC=NC(=C2)N3C(=O)C(=CN3)N4C=CN=N4 |
PubChem CID | 59603622 |
Molecular Weight | 314.3 |
PubChem CID | 59603622 |
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CAS Registry No. | 1154028-82-6 |
BindingDB Ligand | 118339 |
RCSB PDB Ligand | A1H |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
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H2218271 | Certificate of Analysis | Jun 17, 2022 | M413917 |
Solubility | Solubility (25°C) In vitro DMSO: 2 mg/mL warmed with 50ºC Water: bath (6.36 mM); 5%TFA 1.67 mg/mL (5.31 mM); Water: Insoluble; |
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DMSO(mg / mL) Max Solubility | 3 |
DMSO(mM) Max Solubility | 9.545020681 |
Water(mg / mL) Max Solubility | <1 |
Pictogram(s) | GHS08, GHS07 |
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Signal | Danger |
Hazard Statements | H302:Harmful if swallowed H372:Causes damage to organs through prolonged or repeated exposure H360:May damage fertility or the unborn child |
Precautionary Statements | P280:Wear protective gloves/protective clothing/eye protection/face protection. P405:Store locked up. P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P260:Do not breathe dust/fume/gas/mist/vapors/spray. P270:Do not eat, drink or smoke when using this product. P330:Rinse mouth. P203:Obtain, read and follow all safety instructions before use. P301+P317:IF SWALLOWED: Get medical help. P318:if exposed or concerned, get medical advice. P319:Get medical help if you feel unwell. |
1. Oehme F, Jonghaus W, Narouz-Ott L, Huetter J, Flamme I. (2004) A nonradioactive 96-well plate assay for the detection of hypoxia-inducible factor prolyl hydroxylase activity.. Anal Biochem, 330 (1): (74-80). [PMID:15183764] |
2. Bouchie A. (2013) First-in-class anemia drug takes aim at Amgen's dominion.. Nat Biotechnol, 31 (11): (948-9). [PMID:24213751] |
3. Forristal CE, Levesque JP. (2014) Targeting the hypoxia-sensing pathway in clinical hematology.. Stem Cells Transl Med, 3 (2): (135-40). [PMID:24371328] |