Saclofen | CAS#125464-42-8 | GABAB antagonist

MedKoo Cat#: 526402 | Name: Saclofen

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Description:

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

Saclofen is a selective antagonist of GABAB receptors.

Chemical Structure

Saclofen

CAS#125464-42-8

Theoretical Analysis

MedKoo Cat#: 526402

Name: Saclofen

CAS#: 125464-42-8

Chemical Formula: C9H12ClNO3S

Exact Mass: 249.0226

Molecular Weight: 249.71

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 450.00
10mg	USD 750.00
25mg	USD 1,250.00
50mg	USD 1,700.00

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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

Product Data

Instruction

View handling instruction

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/

	Solvent	mg/mL	mM
Solubility
	Water	10.0	40.05

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 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.

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: Chang CH. Lateral orbitofrontal cortical modulation on medial prefrontal cortex-amygdala pathway: Differential regulation of intra-amygdala GABAA and GABAB receptors. Int J Neuropsychopharmacol. 2017 Apr 22. doi: 10.1093/ijnp/pyx027. [Epub ahead of print] PubMed PMID: 28444246. 2: Hu C, Zhao YT, Zhang G, Xu MF. Antinociceptive effects of fucoidan in rat models of vincristine-induced neuropathic pain. Mol Med Rep. 2017 Feb;15(2):975-980. doi: 10.3892/mmr.2016.6071. Epub 2016 Dec 23. PubMed PMID: 28035379. 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. 4: Bassi GS, do C Malvar D, Cunha TM, Cunha FQ, Kanashiro A. Spinal GABA-B receptor modulates neutrophil recruitment to the knee joint in zymosan-induced arthritis. Naunyn Schmiedebergs Arch Pharmacol. 2016 Aug;389(8):851-61. doi: 10.1007/s00210-016-1248-0. Epub 2016 Apr 23. PubMed PMID: 27106212. 5: Sallam MY, El-Gowilly SM, Abdel-Galil AG, El-Mas MM. Central GABAA receptors are involved in inflammatory and cardiovascular consequences of endotoxemia in conscious rats. Naunyn Schmiedebergs Arch Pharmacol. 2016 Mar;389(3):279-88. doi: 10.1007/s00210-015-1201-7. Epub 2015 Dec 21. PubMed PMID: 26685896. 6: Pozdnyakova N, Dudarenko M, Borisova T. New effects of GABAB receptor allosteric modulator rac-BHFF on ambient GABA, uptake/release, Em and synaptic vesicle acidification in nerve terminals. Neuroscience. 2015 Sep 24;304:60-70. doi: 10.1016/j.neuroscience.2015.07.037. Epub 2015 Jul 18. PubMed PMID: 26197223. 7: Jin R, Liu H, Jin WZ, Shi JD, Jin QH, Chu CP, Qiu DL. Propofol depresses cerebellar Purkinje cell activity via activation of GABA(A) and glycine receptors in vivo in mice. Eur J Pharmacol. 2015 Oct 5;764:87-93. doi: 10.1016/j.ejphar.2015.06.052. Epub 2015 Jun 30. PubMed PMID: 26142083. 8: Harte-Hargrove LC, Varga-Wesson A, Duffy AM, Milner TA, Scharfman HE. Opioid receptor-dependent sex differences in synaptic plasticity in the hippocampal mossy fiber pathway of the adult rat. J Neurosci. 2015 Jan 28;35(4):1723-38. doi: 10.1523/JNEUROSCI.0820-14.2015. PubMed PMID: 25632146; PubMed Central PMCID: PMC4308610. 9: Takeda M, Nasu M, Kanazawa T, Shimazu Y. Activation of GABA(B) receptors potentiates inward rectifying potassium currents in satellite glial cells from rat trigeminal ganglia: in vivo patch-clamp analysis. Neuroscience. 2015 Mar 12;288:51-8. doi: 10.1016/j.neuroscience.2014.12.024. Epub 2014 Dec 24. PubMed PMID: 25542421. 10: Andrade CA, De Oliveira LB, Andrade-Franzé GM, De Luca LA Jr, Colombari DS, Menani JV. Gabaergic and opioid receptors mediate the facilitation of NaCl intake induced by α₂-adrenergic activation in the lateral parabrachial nucleus. Behav Brain Res. 2015 Feb 1;278:535-41. doi: 10.1016/j.bbr.2014.10.007. Epub 2014 Oct 14. PubMed PMID: 25448435. 11: Prud'homme GJ, Glinka Y, Udovyk O, Hasilo C, Paraskevas S, Wang Q. GABA protects pancreatic beta cells against apoptosis by increasing SIRT1 expression and activity. Biochem Biophys Res Commun. 2014 Sep 26;452(3):649-54. doi: 10.1016/j.bbrc.2014.08.135. Epub 2014 Sep 1. PubMed PMID: 25193706. 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. 14: Takeda M, Ikeda M, Takahashi M, Kanazawa T, Nasu M, Matsumoto S. Suppression of ATP-induced excitability in rat small-diameter trigeminal ganglion neurons by activation of GABAB receptor. Brain Res Bull. 2013 Sep;98:155-62. doi: 10.1016/j.brainresbull.2013.08.005. Epub 2013 Sep 1. PubMed PMID: 24004472. 15: Gaucher Q, Huetz C, Gourévitch B, Edeline JM. Cortical inhibition reduces information redundancy at presentation of communication sounds in the primary auditory cortex. J Neurosci. 2013 Jun 26;33(26):10713-28. doi: 10.1523/JNEUROSCI.0079-13.2013. PubMed PMID: 23804094; PubMed Central PMCID: PMC3755176. 16: Hsieh KC, Nguyen D, Siegel JM, Lai YY. New pathways and data on rapid eye movement sleep behaviour disorder in a rat model. Sleep Med. 2013 Aug;14(8):719-28. doi: 10.1016/j.sleep.2012.08.008. Epub 2012 Oct 9. PubMed PMID: 23058690; PubMed Central PMCID: PMC3546264. 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. 18: Kemppainen H, Raivio N, Kiianmaa K. Role for ventral pallidal GABAergic mechanisms in the regulation of ethanol self-administration. Psychopharmacology (Berl). 2012 Sep;223(2):211-21. doi: 10.1007/s00213-012-2709-x. Epub 2012 May 3. PubMed PMID: 22552756. 19: Barchini J, Tchachaghian S, Shamaa F, Jabbur SJ, Meyerson BA, Song Z, Linderoth B, Saadé NE. Spinal segmental and supraspinal mechanisms underlying the pain-relieving effects of spinal cord stimulation: an experimental study in a rat model of neuropathy. Neuroscience. 2012 Jul 26;215:196-208. doi: 10.1016/j.neuroscience.2012.04.057. Epub 2012 Apr 28. PubMed PMID: 22548781. 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.