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MedKoo Cat#: 530317 | Name: RSD-921

Description:

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

RSD-921, also known as PD-123497, sodium channel antagonist potentially used as a local anaesthetic agent. RSD 921 produced similarly potent tonic block of all three wild-type channel isoforms, with EC50 values between 35 and 47 microM, whereas the EC50 for block of the IFMQ3 mutant channel was 110+5.5 microM.

Chemical Structure

RSD-921
RSD-921
CAS#114419-77-1

Theoretical Analysis

MedKoo Cat#: 530317

Name: RSD-921

CAS#: 114419-77-1

Chemical Formula: C21H28N2OS

Exact Mass: 356.1922

Molecular Weight: 356.53

Elemental Analysis: C, 70.75; H, 7.92; N, 7.86; O, 4.49; S, 8.99

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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Related CAS #
No Data
Synonym
RSD-921; RSD 921; RSD921; PD-123497; PD 123497; PD123497; PD-123,497; PD 123,497; PD123,497.
IUPAC/Chemical Name
2-(Benzothiophen-4-yl)-N-methyl-N-((1R,2R)-2-pyrrolidin-1-ylcyclohexyl)acetamide
InChi Key
SYHJZCCNQDFHJQ-RTBURBONSA-N
InChi Code
InChI=1S/C21H28N2OS/c1-22(18-8-2-3-9-19(18)23-12-4-5-13-23)21(24)15-16-7-6-10-20-17(16)11-14-25-20/h6-7,10-11,14,18-19H,2-5,8-9,12-13,15H2,1H3/t18-,19-/m1/s1
SMILES Code
O=C(N(C)[C@H]1[C@H](N2CCCC2)CCCC1)CC3=C4C=CSC4=CC=C3
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 356.53 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: Pugsley MK, Saint DA, Hayes ES, Abraham S, Walker MJ. An examination of the cardiac actions of PD117,302, a κ-opioid receptor agonist. Eur J Pharmacol. 2015 Aug 15;761:330-40. doi: 10.1016/j.ejphar.2015.06.018. PubMed PMID: 26086860. 2: Gullapalli S, Ramarao P. L-type Ca2+ channel modulation by dihydropyridines potentiates kappa-opioid receptor agonist induced acute analgesia and inhibits development of tolerance in rats. Neuropharmacology. 2002 Mar;42(4):467-75. PubMed PMID: 11955518. 3: Ribeiro W, Ifa DR, Corso G, Salmon J, Moraes LA, Eberlin MN, de Nucci G. Determination of RSD921 in human plasma by high-performance liquid chromatography-tandem mass spectrometry using tri-deuterated RSD921 as internal standard: application to a phase I clinical trial. J Mass Spectrom. 2001 Oct;36(10):1133-9. PubMed PMID: 11747107. 4: Nemmani KV, Gullapalli S, Ramarao P. Potentiation of kappa-opioid receptor agonist-induced analgesia and hypothermia by fluoxetine. Pharmacol Biochem Behav. 2001 May-Jun;69(1-2):189-93. PubMed PMID: 11420085. 5: Carey GJ, Bergman J. Enadoline discrimination in squirrel monkeys: effects of opioid agonists and antagonists. J Pharmacol Exp Ther. 2001 Apr;297(1):215-23. PubMed PMID: 11259547. 6: Sheridan RD. Quantification of state-dependent drug interactions with the sodium channel. Br J Pharmacol. 2000 Jan;129(2):409-11. PubMed PMID: 10694250; PubMed Central PMCID: PMC1571825. 7: Powell KR, Holtzman SG. Differential antagonism of the rate-decreasing effects of kappa-opioid receptor agonists by naltrexone and norbinaltorphimine. Eur J Pharmacol. 1999 Jul 14;377(1):21-8. PubMed PMID: 10448921. 8: Pugsley MK, Goldin AL. Molecular analysis of the Na+ channel blocking actions of the novel class I anti-arrhythmic agent RSD 921. Br J Pharmacol. 1999 May;127(1):9-18. PubMed PMID: 10369450; PubMed Central PMCID: PMC1565975. 9: Pugsley MK, Goldin AL. Time- and voltage-dependent block of sodium channels expressed in Xenopus oocytes by RSD 921, a novel class I antiarrhythmic drug. Proc West Pharmacol Soc. 1998;41:75-6. PubMed PMID: 9836249. 10: Wilson JL, Walker JS, Antoon JS, Perry MA. Intercellular adhesion molecule-1 expression in adjuvant arthritis in rats: inhibition by kappa-opioid agonist but not by NSAID. J Rheumatol. 1998 Mar;25(3):499-505. PubMed PMID: 9517771. 11: Tortella FC, Rose J, Robles L, Moreton JE, Hughes J, Hunter JC. EEG spectral analysis of the neuroprotective kappa opioids enadoline and PD117302. J Pharmacol Exp Ther. 1997 Jul;282(1):286-93. PubMed PMID: 9223566. 12: Friese N, Chevalier E, Angel F, Pascaud X, Junien JL, Dahl SG, Riviere PJ. Reversal by kappa-agonists of peritoneal irritation-induced ileus and visceral pain in rats. Life Sci. 1997;60(9):625-34. PubMed PMID: 9048965. 13: Wettstein JG, Grouhel A. Opioid antagonist profile of SC nor-binaltorphimine in the formalin paw assay. Pharmacol Biochem Behav. 1996 Feb;53(2):411-6. PubMed PMID: 8808151. 14: Walker ML, Wall RA, Walker MJ. Determination of an arylacetamide antiarrhythmic in rat blood and tissues using reversed-phase high-performance liquid chromatography. J Chromatogr B Biomed Appl. 1996 Jan 26;675(2):257-63. PubMed PMID: 8852713. 15: Shukla VK, Turndorf H, Bansinath M. Pertussis and cholera toxins modulate kappa-opioid receptor agonists-induced hypothermia and gut inhibition. Eur J Pharmacol. 1995 Mar 16;292(3-4):293-9. PubMed PMID: 7796869. 16: Nagasaka H, Yaksh TL. Effects of intrathecal mu, delta, and kappa agonists on thermally evoked cardiovascular and nociceptive reflexes in halothane-anesthetized rats. Anesth Analg. 1995 Mar;80(3):437-43. PubMed PMID: 7864404. 17: Przewłocka B, Lasoń W, Machelska H, van Luijtelaar G, Coenen A, Przewłocki R. Kappa opioid receptor agonists suppress absence seizures in WAG/Rij rats. Neurosci Lett. 1995 Feb 17;186(2-3):131-4. PubMed PMID: 7777181. 18: Pugsley MK, Hayes ES, Saint DA, Walker MJ. Do related kappa agonists produce similar effects on cardiac ion channels? Proc West Pharmacol Soc. 1995;38:25-7. PubMed PMID: 7480011. 19: Langlois A, Diop L, Rivière PJ, Pascaud X, Junien JL. Effect of fedotozine on the cardiovascular pain reflex induced by distension of the irritated colon in the anesthetized rat. Eur J Pharmacol. 1994 Dec 27;271(2-3):245-51. PubMed PMID: 7705424. 20: Przewłocka B, Machelska H, Lasoń W. Kappa opioid receptor agonists inhibit the pilocarpine-induced seizures and toxicity in the mouse. Eur Neuropsychopharmacol. 1994 Dec;4(4):527-33. PubMed PMID: 7894264.

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