S38093 free base | CAS#862896-30-8 | H3 inverse agonist

MedKoo Cat#: 555223 | Name: S38093 free base

Description:

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

S38093 is an inverse agonist at histamine H3 receptors. S38093 has no affinity for other histaminergic receptors.

Chemical Structure

S38093 free base

CAS#862896-30-8 (free base)

Theoretical Analysis

MedKoo Cat#: 555223

Name: S38093 free base

CAS#: 862896-30-8 (free base)

Chemical Formula: C17H24N2O2

Exact Mass: 288.1838

Molecular Weight: 288.39

Elemental Analysis: C, 70.80; H, 8.39; N, 9.71; O, 11.10

Price and Availability

Size	Price	Availability
1mg	USD 300.00	2 Weeks
5mg	USD 550.00	2 Weeks
10mg	USD 750.00	2 Weeks

Bulk Inquiry

Buy Now

Add to Cart

Related CAS #

862896-30-8 (free base) 1222097-72-4 (HCl)

Synonym

S38093 free base; S-38093; S 38093;

IUPAC/Chemical Name

4-(3-(hexahydrocyclopenta[c]pyrrol-2(1H)-yl)propoxy)benzamide

InChi Key

MRNMYWNBLVJWKG-UHFFFAOYSA-N

InChi Code

InChI=1S/C17H24N2O2/c18-17(20)13-5-7-16(8-6-13)21-10-2-9-19-11-14-3-1-4-15(14)12-19/h5-8,14-15H,1-4,9-12H2,(H2,18,20)

SMILES Code

C1=C(OCCCN2CC3CCCC3C2)C=CC(C(=O)N)=C1

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 and ethanol

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:

S38093 has a moderate affinity for rat, mouse and human H3 receptors (Ki = 8.8, 1.44 and 1.2 μM, respectively) and no affinity for other histaminergic receptors.

In vitro activity:

In cellular models, S38093 antagonized mice H3 receptors (KB=0.65µM) and to suppressed cAMP decrease induced by an H3 agonist via human H3 receptors (KB=0.11µM). In cells expressing a high H3 density, S38093 behaved as a moderate inverse agonist at rat and human H3 receptors (EC50=9 and 1.7µM, respectively). Reference: Eur J Pharmacol. 2017 May 15;803:11-23. https://pubmed.ncbi.nlm.nih.gov/28336400/

In vivo activity:

S38093, a new H3 antagonist/inverse agonist, displays antiallodynic and antihyperalgesic effect in neuropathic pain, especially in oxaliplatin-induced neuropathy after chronic administration. S38093 exhibited a significant antihyperalgesic effect in the Streptozocin-induced diabetic (STZ) neuropathy model. Acute S38093 administration displayed a significant cold antiallodynic effect in a model of acute or repeated administration of oxaliplatin-induced neuropathy. Reference: Eur J Pain. 2018 Jan;22(1):127-141. https://pubmed.ncbi.nlm.nih.gov/28877402/

	Solvent	mg/mL	mM
Solubility
	DMSO	57.0	197.66
	Ethanol	57.0	197.66

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 288.39 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.

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:

1. Sors A, Panayi F, Bert L, Favale D, Nosjean O, Audinot V, Arrang JM, Buisson B, Steidl E, Delbos JM, Huhtala T, Kontkanen O, Chollet AM, Casara P, Lestage P. Mechanistic characterization of S 38093, a novel inverse agonist at histamine H3 receptors. Eur J Pharmacol. 2017 May 15;803:11-23. doi: 10.1016/j.ejphar.2017.03.013. Epub 2017 Mar 21. PMID: 28336400. 2. Chaumette T, Chapuy E, Berrocoso E, Llorca-Torralba M, Bravo L, Mico JA, Chalus M, Eschalier A, Ardid D, Marchand F, Sors A. Effects of S 38093, an antagonist/inverse agonist of histamine H3 receptors, in models of neuropathic pain in rats. Eur J Pain. 2018 Jan;22(1):127-141. doi: 10.1002/ejp.1097. Epub 2017 Sep 6. PMID: 28877402. 3. Guilloux JP, Samuels BA, Mendez-David I, Hu A, Levinstein M, Faye C, Mekiri M, Mocaer E, Gardier AM, Hen R, Sors A, David DJ. S 38093, a histamine H3 antagonist/inverse agonist, promotes hippocampal neurogenesis and improves context discrimination task in aged mice. Sci Rep. 2017 Feb 20;7:42946. doi: 10.1038/srep42946. PMID: 28218311; PMCID: PMC5317168.

In vitro protocol:

In vivo protocol:

1. Chaumette T, Chapuy E, Berrocoso E, Llorca-Torralba M, Bravo L, Mico JA, Chalus M, Eschalier A, Ardid D, Marchand F, Sors A. Effects of S 38093, an antagonist/inverse agonist of histamine H3 receptors, in models of neuropathic pain in rats. Eur J Pain. 2018 Jan;22(1):127-141. doi: 10.1002/ejp.1097. Epub 2017 Sep 6. PMID: 28877402. 2. Guilloux JP, Samuels BA, Mendez-David I, Hu A, Levinstein M, Faye C, Mekiri M, Mocaer E, Gardier AM, Hen R, Sors A, David DJ. S 38093, a histamine H3 antagonist/inverse agonist, promotes hippocampal neurogenesis and improves context discrimination task in aged mice. Sci Rep. 2017 Feb 20;7:42946. doi: 10.1038/srep42946. PMID: 28218311; PMCID: PMC5317168.

1: Chaumette T, Chapuy E, Berrocoso E, Llorca-Torralba M, Bravo L, Mico JA, Chalus M, Eschalier A, Ardid D, Marchand F, Sors A. Effects of S 38093, an antagonist/inverse agonist of histamine H3 receptors, in models of neuropathic pain in rats. Eur J Pain. 2018 Jan;22(1):127-141. doi: 10.1002/ejp.1097. Epub 2017 Sep 6. PubMed PMID: 28877402. 2: Sors A, Panayi F, Bert L, Favale D, Nosjean O, Audinot V, Arrang JM, Buisson B, Steidl E, Delbos JM, Huhtala T, Kontkanen O, Chollet AM, Casara P, Lestage P. Mechanistic characterization of S 38093, a novel inverse agonist at histamine H3 receptors. Eur J Pharmacol. 2017 May 15;803:11-23. doi: 10.1016/j.ejphar.2017.03.013. Epub 2017 Mar 21. PubMed PMID: 28336400. 3: Panayi F, Sors A, Bert L, Martin B, Rollin-Jego G, Billiras R, Carrié I, Albinet K, Danober L, Rogez N, Thomas JY, Pira L, Bertaina-Anglade V, Lestage P. In vivo pharmacological profile of S 38093, a novel histamine H3 receptor inverse agonist. Eur J Pharmacol. 2017 May 15;803:1-10. doi: 10.1016/j.ejphar.2017.03.008. Epub 2017 Mar 14. PubMed PMID: 28315340. 4: Guilloux JP, Samuels BA, Mendez-David I, Hu A, Levinstein M, Faye C, Mekiri M, Mocaer E, Gardier AM, Hen R, Sors A, David DJ. S 38093, a histamine H(3) antagonist/inverse agonist, promotes hippocampal neurogenesis and improves context discrimination task in aged mice. Sci Rep. 2017 Feb 20;7:42946. doi: 10.1038/srep42946. PubMed PMID: 28218311; PubMed Central PMCID: PMC5317168. 5: Sors A, Krazem A, Kehr J, Yoshitake T, Dominguez G, Henkous N, Letondor C, Mocaer E, Béracochéa DJ. The Synergistic Enhancing-Memory Effect of Donepezil and S 38093 (a Histamine H(3) Antagonist) Is Mediated by Increased Neural Activity in the Septo-hippocampal Circuitry in Middle-Aged Mice. Front Pharmacol. 2016 Dec 22;7:492. doi: 10.3389/fphar.2016.00492. eCollection 2016. PubMed PMID: 28066242; PubMed Central PMCID: PMC5177663. 6: Palaric C, Pilard S, Fontaine JX, Boccard J, Mathiron D, Rigaud S, Cailleu D, Mesnard F, Gut Y, Renaud T, Petit A, Beaumal JY, Molinié R. Processing of NMR and MS metabolomics data using chemometrics methods: a global tool for fungi biotransformation reactions monitoring. Metabolomics. 2019 Jul 25;15(8):107. doi: 10.1007/s11306-019-1567-5. PMID: 31346787.