MedKoo Cat#: 575975 | Name: GR-127935

Description:

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

GR-127935 is a potent and selective 5-HT1B/1D receptor antagonist.

Chemical Structure

GR-127935
GR-127935
CAS#148672-13-3 (free base)

Theoretical Analysis

MedKoo Cat#: 575975

Name: GR-127935

CAS#: 148672-13-3 (free base)

Chemical Formula: C29H31N5O3

Exact Mass: 497.2427

Molecular Weight: 497.60

Elemental Analysis: C, 70.00; H, 6.28; N, 14.07; O, 9.65

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Synonym
GR 127935; GR127935; GR-127935
IUPAC/Chemical Name
(1,1'-Biphenyl)-4-carboxamide, N-(4-methoxy-3-(4-methyl-1-piperazinyl)phenyl)-2'-methyl-4'-(5-methyl-1,2,4-oxadiazol-3-yl)-
InChi Key
YDBCEBYHYKAFRX-UHFFFAOYSA-N
InChi Code
InChI=1S/C29H31N5O3/c1-19-17-23(28-30-20(2)37-32-28)9-11-25(19)21-5-7-22(8-6-21)29(35)31-24-10-12-27(36-4)26(18-24)34-15-13-33(3)14-16-34/h5-12,17-18H,13-16H2,1-4H3,(H,31,35)
SMILES Code
COc1ccc(NC(=O)c2ccc(cc2)c3ccc(cc3C)c4noc(C)n4)cc1N5CCN(C)CC5
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

Preparing Stock Solutions

The following data is based on the product molecular weight 497.60 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
1: Sánchez-Maldonado C, López-Sánchez P, Anguiano-Robledo L, Leopoldo M, Lacivita E, Terrón JA. GR-127935-sensitive mechanism mediating hypotension in anesthetized rats: are 5-HT5B receptors involved? J Cardiovasc Pharmacol. 2015 Apr;65(4):335-41. doi: 10.1097/FJC.0000000000000200. PubMed PMID: 25502305. 2: Uphouse L, Hiegel C, Guptarak J, Maswood N. Progesterone reduces the effect of the serotonin 1B/1D receptor antagonist, GR 127935, on lordosis behavior. Horm Behav. 2009 Jan;55(1):169-74. doi: 10.1016/j.yhbeh.2008.09.011. PubMed PMID: 18952090; PubMed Central PMCID: PMC2665997. 3: Chaouloff F, Courvoisier H, Moisan MP, Mormède P. GR 127935 reduces basal locomotor activity and prevents RU 24969-, but not D-amphetamine-induced hyperlocomotion, in the Wistar-Kyoto hyperactive (WKHA) rat. Psychopharmacology (Berl). 1999 Jan;141(3):326-31. PubMed PMID: 10027515. 4: Harrison AA, Parsons LH, Koob GF, Markou A. RU 24969, a 5-HT1A/1B agonist, elevates brain stimulation reward thresholds: an effect reversed by GR 127935, a 5-HT1B/1D antagonist. Psychopharmacology (Berl). 1999 Jan;141(3):242-50. PubMed PMID: 10027505. 5: Chaouloff F, Aguerre S, Mormede P. GR 127935 and (+)-WAY 100135 do not affect TFMPP-induced inhibition of 5-HT synthesis in the midbrain and hippocampus of Wistar-Kyoto rats. Neuropharmacology. 1998 Sep;37(9):1159-67. PubMed PMID: 9833646.