WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H319678
CAS#: 757950-09-7
Description: Raseglurant, aslo known as ADX-10059, is a negative allosteric modulator of the mGlu5 receptor and derivative of MPEP which was under development by Addex Therapeutics for the treatment of migraine, gastroesophageal reflux disease, and dental anxiety. It reached phase II clinical trials for all of the aforementioned indications before being discontinued due to the observation of possible predictive signs of hepatotoxicity in patients with long-term use.
Hodoodo Cat#: H319678
Name: Raseglurant
CAS#: 757950-09-7
Chemical Formula: C15H13FN2
Exact Mass: 240.11
Molecular Weight: 240.281
Elemental Analysis: C, 74.98; H, 5.45; F, 7.91; N, 11.66
Synonym: ADX-10059; ADX 10059; ADX10059; Raseglurant
IUPAC/Chemical Name: 2-[(3-Fluorophenyl)ethynyl]-4,6-dimethyl-3-pyridinamine
InChi Key: MEDCLNYIYBERKO-UHFFFAOYSA-N
InChi Code: InChI=1S/C15H13FN2/c1-10-8-11(2)18-14(15(10)17)7-6-12-4-3-5-13(16)9-12/h3-5,8-9H,17H2,1-2H3
SMILES Code: NC1=C(C)C=C(C)N=C1C#CC2=CC=CC(F)=C2
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
More Info:
| Biological target: | |
| In vitro activity: | |
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The following data is based on the product molecular weight 240.28 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 |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Marin JC, Goadsby PJ. Glutamatergic fine tuning with ADX-10059: a novel
therapeutic approach for migraine? Expert Opin Investig Drugs. 2010
Apr;19(4):555-61. doi: 10.1517/13543781003691832. Review. PubMed PMID: 20218930.
2: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin
Pharmacol. 2009 Dec;31(10):661-700. PubMed PMID: 20140276.
