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MedKoo Cat#: 326953 | Name: Pagoclone
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Description:

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

Pagoclone, also known as CI-1043; IP-456; RP-62955; RP-59037, is a GABA receptor agonist potentially for the treatment of stuttering, panic disorder and generalised anxiety. It binds with roughly equivalent high affinity (0.7–9.1 nM) to the benzodiazepine binding site of human GABAA receptors containing either an α1, α2, α3 or α5 subunit. It is a partial agonist at α1-, α2- and α5-containing GABAA receptors and a full agonist at receptors containing an α3 subunit.

Chemical Structure

Pagoclone
Pagoclone
CAS#133737-32-3

Theoretical Analysis

MedKoo Cat#: 326953

Name: Pagoclone

CAS#: 133737-32-3

Chemical Formula: C23H22ClN3O2

Exact Mass: 407.1401

Molecular Weight: 407.90

Elemental Analysis: C, 67.73; H, 5.44; Cl, 8.69; N, 10.30; O, 7.84

Price and Availability

Size Price Availability Quantity
5mg USD 325.00
25mg USD 950.00
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Related CAS #
No Data
Synonym
Pagoclone; CI-1043; IP-456; RP-62955; RP-59037; CI1043; IP456; RP62955; RP59037. Bextra.
IUPAC/Chemical Name
2-(7-chloro-1,8-naphthyridin-2-yl)-3-(5-methyl-2-oxohexyl)isoindolin-1-one
InChi Key
HIUPRQPBWVEQJJ-UHFFFAOYSA-N
InChi Code
InChI=1S/C23H22ClN3O2/c1-14(2)7-10-16(28)13-19-17-5-3-4-6-18(17)23(29)27(19)21-12-9-15-8-11-20(24)25-22(15)26-21/h3-6,8-9,11-12,14,19H,7,10,13H2,1-2H3
SMILES Code
O=C1N(C2=NC3=NC(Cl)=CC=C3C=C2)C(CC(CCC(C)C)=O)C4=C1C=CC=C4
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
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Pagoclone, also known as CI-1043; IP-456; RP-62955; RP-59037, is a GABA receptor agonist.
In vitro activity:
TBD
In vivo activity:
TBD
Solvent mg/mL mM
Solubility
DMSO 10.0 24.52
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 407.90 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
Formulation protocol:
TBD
In vitro protocol:
TBD
In vivo protocol:
TBD
1: Kronstrand R, Roman M, Johansson A, Wu X, Green H, Truver MT. Rilmazafone: A designer benzodiazepine pro-drug involved in fatal intoxications. J Anal Toxicol. 2023 Sep 15;47(7):640-643. doi: 10.1093/jat/bkad041. PMID: 37348041. 2: Li XH, Gong JF, Song MP. Diastereoselective synthesis of chiral 3-substituted isoindolinones via rhodium(III)-catalyzed oxidative C-H olefination/annulation. Org Biomol Chem. 2021 Jul 7;19(26):5876-5887. doi: 10.1039/d1ob00656h. Erratum in: Org Biomol Chem. 2021 Jul 7;19(26):5914. doi: 10.1039/d1ob90092g. PMID: 34126629. 3: Zhang Y, Zhu H, Huang Y, Hu Q, He Y, Wen Y, Zhu G. Multicomponent Synthesis of Isoindolinones by RhIII Relay Catalysis: Synthesis of Pagoclone and Pazinaclone from Benzaldehyde. Org Lett. 2019 Mar 1;21(5):1273-1277. doi: 10.1021/acs.orglett.8b04026. Epub 2019 Feb 12. PMID: 30747539. 4: Ingham RJ. Comments on article by Maguire et al: pagoclone trial: questionable findings for stuttering treatment. J Clin Psychopharmacol. 2010 Oct;30(5):649-50; author reply 650-1. doi: 10.1097/JCP.0b013e3181f1f130. PMID: 20841975. 5: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2010 Jun;32(5):331-88. doi: 10.1358/mf.2010.32.5.1520420. PMID: 20664824. 6: Maguire G, Franklin D, Vatakis NG, Morgenshtern E, Denko T, Yaruss JS, Spotts C, Davis L, Davis A, Fox P, Soni P, Blomgren M, Silverman A, Riley G. Exploratory randomized clinical study of pagoclone in persistent developmental stuttering: the EXamining Pagoclone for peRsistent dEvelopmental Stuttering Study. J Clin Psychopharmacol. 2010 Feb;30(1):48-56. doi: 10.1097/JCP.0b013e3181caebbe. PMID: 20075648. 7: Caveney AF, Giordani B, Haig GM. Preliminary effects of pagoclone, a partial GABA(A) agonist, on neuropsychological performance. Neuropsychiatr Dis Treat. 2008 Feb;4(1):277-82. doi: 10.2147/ndt.s2351. PMID: 18728798; PMCID: PMC2515892. 8: Bayes M. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2007 Mar;29(2):153-73. PMID: 17440629. 9: de Wit H, Vicini L, Haig GM, Hunt T, Feltner D. Evaluation of the abuse potential of pagoclone, a partial GABAA agonist. J Clin Psychopharmacol. 2006 Jun;26(3):268-73. doi: 10.1097/01.jcp.0000218983.61683.96. PMID: 16702891. 10: Atack JR, Pike A, Marshall G, Stanley J, Lincoln R, Cook SM, Lewis RT, Blackaby WP, Goodacre SC, McKernan RM, Dawson GR, Wafford KA, Reynolds DS. The in vivo properties of pagoclone in rat are most likely mediated by 5'-hydroxy pagoclone. Neuropharmacology. 2006 May;50(6):677-89. doi: 10.1016/j.neuropharm.2005.11.014. Epub 2006 Jan 20. PMID: 16430927. 11: Lingford-Hughes A, Wilson SJ, Feeney A, Grasby PG, Nutt DJ. A proof-of- concept study using [11C]flumazenil PET to demonstrate that pagoclone is a partial agonist. Psychopharmacology (Berl). 2005 Aug;180(4):789-91. doi: 10.1007/s00213-005-0060-1. Epub 2005 Sep 14. PMID: 15986186. 12: Atack JR. The benzodiazepine binding site of GABA(A) receptors as a target for the development of novel anxiolytics. Expert Opin Investig Drugs. 2005 May;14(5):601-18. doi: 10.1517/13543784.14.5.601. PMID: 15926867. 13: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2004 Apr;26(3):211-44. PMID: 15148527. 14: Atack JR. Anxioselective compounds acting at the GABA(A) receptor benzodiazepine binding site. Curr Drug Targets CNS Neurol Disord. 2003 Aug;2(4):213-32. doi: 10.2174/1568007033482841. PMID: 12871032. 15: Bateson A. Pagoclone Indevus. Curr Opin Investig Drugs. 2003 Jan;4(1):91-5. PMID: 12625036. 16: Sandford JJ, Forshall S, Bell C, Argyropoulos S, Rich A, D'Orlando KJ, Gammans RE, Nutt DJ. Crossover trial of pagoclone and placebo in patients with DSM-IV panic disorder. J Psychopharmacol. 2001 Sep;15(3):205-8. doi: 10.1177/026988110101500312. PMID: 11565630.