MedKoo Cat#: 461059 | Name: RU5135 HCl

Description:

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

RU 5135 is a GABA steroid antagonist.

Chemical Structure

RU5135 HCl
RU5135 HCl
CAS#78774-26-2

Theoretical Analysis

MedKoo Cat#: 461059

Name: RU5135 HCl

CAS#: 78774-26-2

Chemical Formula: C18H30Cl2N2O2

Exact Mass:

Molecular Weight: 377.35

Elemental Analysis: Chemical Formula: C18H30Cl2N2O2 Exact Mass: 376.1684 Molecular Weight: 377.3500 Elemental Analysis: C, 57.29; H, 8.01; Cl, 18.79; N, 7.42; O, 8.48

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 #
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Synonym
RU 5135; R-5135; R5135; R 5135; RU-5135; RU5135; RU5135 HCl;
IUPAC/Chemical Name
(3aS,3bS,5aR,7R,9aS,9bS,11aS)-2-amino-7-hydroxy-9a,11a-dimethyl-3,3a,3b,4,5,5a,6,7,8,9,9a,9b,11,11a-tetradecahydro-10H-naphtho[2,1-e]indol-10-one dihydrochloride
InChi Key
LMJVOVNZZBBMND-LNRUUEQNSA-N
InChi Code
InChI=1S/C18H28N2O2.2ClH/c1-17-6-5-11(21)7-10(17)3-4-12-13-8-15(19)20-18(13,2)9-14(22)16(12)17;;/h10-13,16,21H,3-9H2,1-2H3,(H2,19,20);2*1H/t10-,11-,12+,13+,16-,17+,18+;;/m1../s1
SMILES Code
O=C1[C@@]2([H])[C@](CC[C@]3([H])C[C@H](O)CC[C@@]32C)([H])[C@]4([H])CC(N)=N[C@@]4(C)C1.[H]Cl.[H]Cl
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
>3 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 377.35 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: Curtis DR, Malik R. Glycine antagonism by RU 5135. Eur J Pharmacol. 1985 Apr 16;110(3):383-4. PubMed PMID: 4007055. 2: Myslobodsky MS, Mintz M, Tarrasch R, Bar-Ziv J. A steroid derivative (RU 5135) exhibits epileptogenicity in the presence of deficient blood-brain barrier. Pharmacol Biochem Behav. 1991 Feb;38(2):327-31. PubMed PMID: 2057502. 3: Cadoni C, Gee KW. Complex interactions between the steroid derivative RU 5135 and the GABAA-receptor complex. Eur J Pharmacol. 1992 Oct 1;227(2):147-51. PubMed PMID: 1330646. 4: Hunt P, Clements-Jewery S. A steroid derivative, R 5135, antagonizes the GABA/benzodiazepine receptor interaction. Neuropharmacology. 1981 Apr;20(4):357-61. PubMed PMID: 6270588. 5: Kofman O, Tarrasch R, Mintz M, Myslobodsky MS. Epileptogenic activity in the amygdala is not affected by the amidine steroid, R 5135. Brain Res Bull. 1992 Sep-Oct;29(3-4):511-4. PubMed PMID: 1393623. 6: Myslobodsky MS, Kofman O. Regular and lasting neocortical spiking produced by systemic administration of a steroid derivative in the rat. Neuropharmacology. 1983 Feb;22(2):157-64. PubMed PMID: 6403888. 7: Hawkinson JE, Acosta-Burruel M, Kimbrough CL, Goodnough DB, Wood PL. Steroid inhibition of [3H]SR 95531 binding to the GABAA recognition site. Eur J Pharmacol. 1996 May 23;304(1-3):141-6. PubMed PMID: 8813596. 8: Ong J, Kerr DI. Modulation of spontaneous motility by GABAA receptor antagonism in the guinea pig isolated ileum. Neurosci Lett. 1989 Jun 19;101(2):203-8. PubMed PMID: 2549461. 9: Wong EH, Iversen LL. Modulation of [3H]diazepam binding in rat cortical membranes by GABAA agonists. J Neurochem. 1985 Apr;44(4):1162-7. PubMed PMID: 2983028. 10: Kakemoto E, Okuyama E, Nagata K, Ozoe Y. Interaction of anisatin with rat brain gamma-aminobutyric acidA receptors: allosteric modulation by competitive antagonists. Biochem Pharmacol. 1999 Aug 15;58(4):617-21. PubMed PMID: 10413298. 11: Vaello ML, Ruiz-Gómez A, Mayor F Jr. Glycinergic ligands modulate the rate of phosphorylation of the glycine receptor by protein kinase C. Biochem Biophys Res Commun. 1992 Oct 30;188(2):813-9. PubMed PMID: 1332706. 12: Rognan D, Boulanger T, Hoffmann R, Vercauteren DP, Andre JM, Durant F, Wermuth CG. Structure and molecular modeling of GABAA receptor antagonists. J Med Chem. 1992 May 29;35(11):1969-77. PubMed PMID: 1317920. 13: Korpi ER, Lüddens H, Seeburg PH. GABAA antagonists reveal binding sites for [35S]TBPS in cerebellar granular cell layer. Eur J Pharmacol. 1992 Feb 18;211(3):427-8. PubMed PMID: 1319916. 14: Maksay G, Ticku MK. Diazotization and thiocyanate differentiate agonists from antagonists for the high- and low-affinity receptors of gamma-aminobutyric acid. J Neurochem. 1984 Jul;43(1):261-8. PubMed PMID: 6327917. 15: Olsen RW. gamma-Aminobutyric acid receptor binding antagonism by the amidine steroid RU5135. Eur J Pharmacol. 1984 Aug 17;103(3-4):333-7. PubMed PMID: 6092106. 16: Maksay G, Molnár P, Gruber L. Common modes of action of gamma-butyrolactones and pentylenetetrazol on the GABAA receptor-ionophore complex. Eur J Pharmacol. 1994 Dec 15;288(1):61-8. PubMed PMID: 7705469. 17: Maksay G, Simonyi M. Kinetic modulation by GABAergic agents of high- and low-affinity binding of [3H]methyl beta-carboline-3-carboxylate. J Neurochem. 1988 Jun;50(6):1859-64. PubMed PMID: 2836560. 18: Maksay G. GABAA receptor populations bind agonists and antagonists differentially and with opposite affinities. J Neurochem. 1988 Jun;50(6):1865-71. PubMed PMID: 2836561. 19: Jensen AA. Functional characterisation of human glycine receptors in a fluorescence-based high throughput screening assay. Eur J Pharmacol. 2005 Oct 3;521(1-3):39-42. Epub 2005 Sep 21. PubMed PMID: 16182281. 20: Sattelle DB, Pinnock RD, Wafford KA, David JA. GABA receptors on the cell-body membrane of an identified insect motor neuron. Proc R Soc Lond B Biol Sci. 1988 Jan 22;232(1269):443-56. PubMed PMID: 2451252.