GR 82334

GR 82334 is a potent and specific reversible tachykinin NK1 receptor antagonist. GR 82334 inhibits substance P-induced sensitization by blocking SP NK1 receptors in naked mole-rats.

Product information

CAS Number: 129623-01-4

Molecular Weight: 1386.55

Formula: C69H91N15O16

Chemical Name: (3S)-4-[(2S)-2-{[(1S)-1-{[(1S)-5-amino-1-{[(1S)-1-{[(2S)-1-[(5S)-7-[(1S)-1-{[(1S)-1-carbamoyl-2-(1H-indol-3-yl)ethyl]carbamoyl}-3-methylbutyl]-6-oxo-1,7-diazaspiro[4.4]nonan-1-yl]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]carbamoyl}-2-phenylethyl]carbamoyl}pentyl]carbamoyl}-2-carbamoylethyl]carbamoyl}pyrrolidin-1-yl]-4-oxo-3-[(2S)-2-{[(2S)-5-oxopyrrolidin-2-yl]formamido}propanamido]butanoic acid

Smiles: CC(C)C[C@@H](C(=O)N[C@@H](CC1=CNC2=CC=CC=C12)C(N)=O)N1CC[C@@]2(CCCN2C(=O)[C@H](CC2C=CC(O)=CC=2)NC(=O)[C@H](CC2C=CC=CC=2)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H]2CCC(=O)N2)C1=O

InChiKey: KWECNVXXONDEKG-JTCMYMKESA-N

InChi: InChI=1S/C69H91N15O16/c1-38(2)31-54(65(97)77-48(58(72)90)34-42-37-73-45-16-8-7-15-44(42)45)83-30-26-69(68(83)100)25-12-29-84(69)67(99)51(33-41-19-21-43(85)22-20-41)81-62(94)49(32-40-13-5-4-6-14-40)78-61(93)46(17-9-10-27-70)76-63(95)50(35-55(71)86)79-64(96)53-18-11-28-82(53)66(98)52(36-57(88)89)80-59(91)39(3)74-60(92)47-23-24-56(87)75-47/h4-8,13-16,19-22,37-39,46-54,73,85H,9-12,17-18,23-36,70H2,1-3H3,(H2,71,86)(H2,72,90)(H,74,92)(H,75,87)(H,76,95)(H,77,97)(H,78,93)(H,79,96)(H,80,91)(H,81,94)(H,88,89)/t39-,46-,47-,48-,49-,50-,51-,52-,53-,54-,69-/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vivo:

GR 82334 (intrathecal administration; 0.1 nmol-1 nmol) excites rats unnary bladder motihty at 1 nmol but not at 0.1 nmol, and the reflex chemonociceptive is reduced by the topical application of capsaicin (4 μg/50 ul). GR 82334 (10 nM-1 µM; injected between vertebrae L4 and L5) has no effect at 10 nM in neither species, increases heat-induced foot withdrawal latency in mice at doses >100 nM, but no such increase in naked mole-rats, where doses >100 nM evoke a tendency for decreased latency.

Products are for research use only. Not for human use.