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

MedKoo CAT#: 526402

CAS#: 125464-42-8

Description: Saclofen is a selective antagonist of GABAB receptors.


Chemical Structure

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Saclofen
CAS# 125464-42-8

Theoretical Analysis

MedKoo Cat#: 526402
Name: Saclofen
CAS#: 125464-42-8
Chemical Formula: C9H12ClNO3S
Exact Mass: 249.02
Molecular Weight: 249.710
Elemental Analysis: C, 43.29; H, 4.84; Cl, 14.20; N, 5.61; O, 19.22; S, 12.84

Price and Availability

Size Price Availability Quantity
5mg USD 400
10mg USD 700
25mg USD 1200
50mg USD 1650
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Synonym: Saclofen

IUPAC/Chemical Name: 3-Amino-2-(4-chlorophenyl)propane-1-sulfonic acid

InChi Key: JYLNVJYYQQXNEK-UHFFFAOYSA-N

InChi Code: InChI=1S/C9H12ClNO3S/c10-9-3-1-7(2-4-9)8(5-11)6-15(12,13)14/h1-4,8H,5-6,11H2,(H,12,13,14)

SMILES Code: O=S(CC(C1=CC=C(Cl)C=C1)CN)(O)=O

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:
Biological target: Saclofen is a GABAB receptor antagonist with an IC50 of 7.8 μM.
In vitro activity: To be determined
In vivo activity: Activation of GABAB receptor in the spinal cord may suppress the TLR4/Myd88/NF-κB signaling pathway and alleviate diabetic neuropathic pain (DNP). In a rat model of DNP, intrathecal injection of saclofen decreased paw withdrawal threshold and paw withdrawal thermal latency in DNP rats. Reference: Mediators Inflamm. 2018 Dec 10;2018:6016272. https://pubmed.ncbi.nlm.nih.gov/30647535/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
Water 10.0 40.05

Preparing Stock Solutions

The following data is based on the product molecular weight 249.71 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: 1. Liu P, Yuan HB, Zhao S, Liu FF, Jiang YQ, Guo YX, Wang XL. Activation of GABAB Receptor Suppresses Diabetic Neuropathic Pain through Toll-Like Receptor 4 Signaling Pathway in the Spinal Dorsal Horn. Mediators Inflamm. 2018 Dec 10;2018:6016272. doi: 10.1155/2018/6016272. PMID: 30647535; PMCID: PMC6311757. 2. Li G, Lv J, Wang J, Wan P, Li Y, Jiang H, Jin Q. GABAB receptors in the hippocampal dentate gyrus are involved in spatial learning and memory impairment in a rat model of vascular dementia. Brain Res Bull. 2016 Jun;124:190-7. doi: 10.1016/j.brainresbull.2016.05.006. Epub 2016 May 12. PMID: 27181927.
In vitro protocol: To be determined1. Liu P, Yuan HB, Zhao S, Liu FF, Jiang YQ, Guo YX, Wang XL. Activation of GABAB Receptor Suppresses Diabetic Neuropathic Pain through Toll-Like Receptor 4 Signaling Pathway in the Spinal Dorsal Horn. Mediators Inflamm. 2018 Dec 10;2018:6016272. doi: 10.1155/2018/6016272. PMID: 30647535; PMCID: PMC6311757. 2. Li G, Lv J, Wang J, Wan P, Li Y, Jiang H, Jin Q. GABAB receptors in the hippocampal dentate gyrus are involved in spatial learning and memory impairment in a rat model of vascular dementia. Brain Res Bull. 2016 Jun;124:190-7. doi: 10.1016/j.brainresbull.2016.05.006. Epub 2016 May 12. PMID: 27181927.
In vivo protocol: 1. Liu P, Yuan HB, Zhao S, Liu FF, Jiang YQ, Guo YX, Wang XL. Activation of GABAB Receptor Suppresses Diabetic Neuropathic Pain through Toll-Like Receptor 4 Signaling Pathway in the Spinal Dorsal Horn. Mediators Inflamm. 2018 Dec 10;2018:6016272. doi: 10.1155/2018/6016272. PMID: 30647535; PMCID: PMC6311757. 2. Li G, Lv J, Wang J, Wan P, Li Y, Jiang H, Jin Q. GABAB receptors in the hippocampal dentate gyrus are involved in spatial learning and memory impairment in a rat model of vascular dementia. Brain Res Bull. 2016 Jun;124:190-7. doi: 10.1016/j.brainresbull.2016.05.006. Epub 2016 May 12. PMID: 27181927.

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3: Li G, Lv J, Wang J, Wan P, Li Y, Jiang H, Jin Q. GABAB receptors in the hippocampal dentate gyrus are involved in spatial learning and memory impairment in a rat model of vascular dementia. Brain Res Bull. 2016 Jun;124:190-7. doi: 10.1016/j.brainresbull.2016.05.006. Epub 2016 May 12. PubMed PMID: 27181927.

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12: Liu QY, Wang CY, Cai ZL, Xu ST, Liu WX, Xiao P, Li CH. Effects of intrahippocampal GABAB receptor antagonist treatment on the behavioral long-term potentiation and Y-maze learning performance. Neurobiol Learn Mem. 2014 Oct;114:26-31. doi: 10.1016/j.nlm.2014.04.005. Epub 2014 Apr 20. PubMed PMID: 24758898.

13: Varani AP, Pedrón VT, Bettler B, Balerio GN. Involvement of GABAB receptors in biochemical alterations induced by anxiety-related responses to nicotine in mice: genetic and pharmacological approaches. Neuropharmacology. 2014 Jun;81:31-41. doi: 10.1016/j.neuropharm.2014.01.030. Epub 2014 Jan 30. PubMed PMID: 24486711.

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17: Saadé NE, Al Amin HA, Barchini J, Tchachaghian S, Shamaa F, Jabbur SJ, Atweh SF. Brainstem injection of lidocaine releases the descending pain-inhibitory mechanisms in a rat model of mononeuropathy. Exp Neurol. 2012 Sep;237(1):180-90. doi: 10.1016/j.expneurol.2012.06.021. Epub 2012 Jul 1. PubMed PMID: 22759335.

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20: Varani AP, Balerio GN. GABA(B) receptors involvement in the effects induced by nicotine on anxiety-related behaviour in mice. Pharmacol Res. 2012 May;65(5):507-13. doi: 10.1016/j.phrs.2012.03.001. Epub 2012 Mar 13. PubMed PMID: 22430317.