MedKoo Biosciences, Inc.
Tel:   +1-919-636-5577    Fax:   +1-919-980-4831    Email:   sales@medkoo.com
Search
Login Register
Search
MedKoo Cat#: 574405 | Name: SKF-97541
Featured

Description:

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

SKF-97541 is a GABA-B agonist that is 10-fold more potent than Baclofen. SKF-97541 shows antidepressant effects in animal models and is also a GABAA-ρ antagonist.

Chemical Structure

SKF-97541
SKF-97541
CAS#127729-35-5

Theoretical Analysis

MedKoo Cat#: 574405

Name: SKF-97541

CAS#: 127729-35-5

Chemical Formula: C4H12NO2P

Exact Mass: 137.0606

Molecular Weight: 137.12

Elemental Analysis: C, 35.04; H, 8.82; N, 10.22; O, 23.34; P, 22.59

Price and Availability

Size Price Availability Quantity
10mg USD 550.00 2 Weeks
50mg USD 1,500.00 2 Weeks
Bulk Inquiry
Buy Now
Add to Cart
Related CAS #
No Data
Synonym
SKF97541, SKF 97541, CGP35024, CGP-35024, CGP 35024
IUPAC/Chemical Name
3-Aminopropyl(methyl)phosphinic acid
InChi Key
NHVRIDDXGZPJTJ-UHFFFAOYSA-N
InChi Code
InChI=1S/C4H12NO2P/c1-8(6,7)4-2-3-5/h2-5H2,1H3,(H,6,7)
SMILES Code
O=P(C)(CCCN)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
>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
Product Data
Product Data
Instruction
View handling instruction
Biological target:
SKF-97541 is a potent GABAB agonist (EC50 = 50 nM) and depresses striatal synaptic potentials and hyperpolarizes nigral neurons (EC50 values = 92 nM and 150 nM, respectively).
In vitro activity:
In this study, SKF-97541 did not have a significant impact on the basal or GnRH-induced promoter activity of LHbeta and FSHbeta subunits in the mouse pituitary gonadotroph cell line LbetaT2. Reference: Biol Reprod. 2015 Feb;92(2):45. https://pubmed.ncbi.nlm.nih.gov/25519184/
In vivo activity:
The study investigated the impact of SKF-97541 on epileptic afterdischarges (ADs) in the cortex and hippocampus of adult rats. SKF-97541 prolonged cortical Ads but did not significantly affect hippocampal ADs, indicating a proconvulsant effect in the cortex. The study suggests a distinct role for GABA(B) receptors in these brain structures, with differences in the refractory period for electrically-induced ADs. Reference: Physiol Res. 2014;63(4):529-34. https://pubmed.ncbi.nlm.nih.gov/24702499/
Solvent mg/mL mM comments
Solubility
Water 13.7 100.00
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 137.12 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. Mijiddorj T, Kanasaki H, Sukhbaatar U, Oride A, Kyo S. DS1, a delta subunit-containing GABA(A) receptor agonist, increases gonadotropin subunit gene expression in mouse pituitary gonadotrophs. Biol Reprod. 2015 Feb;92(2):45. doi: 10.1095/biolreprod.114.123893. Epub 2014 Dec 17. PMID: 25519184. 2. Bon C, Galvan M. Electrophysiological actions of GABAB agonists and antagonists in rat dorso-lateral septal neurones in vitro. Br J Pharmacol. 1996 Jun;118(4):961-7. doi: 10.1111/j.1476-5381.1996.tb15493.x. PMID: 8799569; PMCID: PMC1909507. 3. Fábera P, Mareš P. Effect of GABA(B) receptor agonist SKF97541 on cortical and hippocampal epileptic afterdischarges. Physiol Res. 2014;63(4):529-34. doi: 10.33549/physiolres.932699. Epub 2014 Apr 3. PMID: 24702499. 4. Mares P. Anticonvulsant action of GABA-B receptor agonist SKF97541 differs from that of baclofen. Physiol Res. 2008;57(5):789-792. doi: 10.33549/physiolres.931338. Epub 2007 Oct 11. PMID: 17949247.
In vitro protocol:
1. Mijiddorj T, Kanasaki H, Sukhbaatar U, Oride A, Kyo S. DS1, a delta subunit-containing GABA(A) receptor agonist, increases gonadotropin subunit gene expression in mouse pituitary gonadotrophs. Biol Reprod. 2015 Feb;92(2):45. doi: 10.1095/biolreprod.114.123893. Epub 2014 Dec 17. PMID: 25519184. 2. Bon C, Galvan M. Electrophysiological actions of GABAB agonists and antagonists in rat dorso-lateral septal neurones in vitro. Br J Pharmacol. 1996 Jun;118(4):961-7. doi: 10.1111/j.1476-5381.1996.tb15493.x. PMID: 8799569; PMCID: PMC1909507.
In vivo protocol:
1. Fábera P, Mareš P. Effect of GABA(B) receptor agonist SKF97541 on cortical and hippocampal epileptic afterdischarges. Physiol Res. 2014;63(4):529-34. doi: 10.33549/physiolres.932699. Epub 2014 Apr 3. PMID: 24702499. 2. Mares P. Anticonvulsant action of GABA-B receptor agonist SKF97541 differs from that of baclofen. Physiol Res. 2008;57(5):789-792. doi: 10.33549/physiolres.931338. Epub 2007 Oct 11. PMID: 17949247.
1: Chapman RW, Danko G, del Prado M, Egan RW, Kreutner W, Rizzo CA, Hey JA. Further evidence for prejunctional GABA-B inhibition of cholinergic and peptidergic bronchoconstriction in guinea pigs: studies with new agonists and antagonists. Pharmacology. 1993 Jun;46(6):315-23. doi: 10.1159/000139062. PMID: 8390694. 2: Hashimoto T, Kuriyama K. In vivo evidence that GABA(B) receptors are negatively coupled to adenylate cyclase in rat striatum. J Neurochem. 1997 Jul;69(1):365-70. doi: 10.1046/j.1471-4159.1997.69010365.x. PMID: 9202330. 3: Wettstein JG, Host M, Hitchcock JM. Selectivity of action of typical and atypical anti-psychotic drugs as antagonists of the behavioral effects of 1-[2,5-dimethoxy-4-iodophenyl]-2-aminopropane (DOI). Prog Neuropsychopharmacol Biol Psychiatry. 1999 Apr;23(3):533-44. doi: 10.1016/s0278-5846(99)00014-7. PMID: 10378235. 4: Blackshaw LA, Staunton E, Lehmann A, Dent J. Inhibition of transient LES relaxations and reflux in ferrets by GABA receptor agonists. Am J Physiol. 1999 Oct;277(4):G867-74. doi: 10.1152/ajpgi.1999.277.4.G867. PMID: 10516154. 5: Bräuner-Osborne H, Krogsgaard-Larsen P. Functional pharmacology of cloned heterodimeric GABAB receptors expressed in mammalian cells. Br J Pharmacol. 1999 Dec;128(7):1370-4. doi: 10.1038/sj.bjp.0702914. PMID: 10602314; PMCID: PMC1571770. 6: Jackson GL, Kuehl D. The GABA(B) antagonist CGP 52432 attenuates the stimulatory effect of the GABA(B) agonist SKF 97541 on luteinizing hormone secretion in the male sheep. Exp Biol Med (Maywood). 2002 May;227(5):315-20. doi: 10.1177/153537020222700503. PMID: 11976401. 7: Kerr DI, Ong J, Puspawati NM, Prager RH. Arylalkylamines are a novel class of positive allosteric modulators at GABA(B) receptors in rat neocortex. Eur J Pharmacol. 2002 Sep 6;451(1):69-77. doi: 10.1016/s0014-2999(02)02195-7. PMID: 12223231. 8: Sokolova E, Nistri A, Giniatullin R. The ATP-mediated fast current of rat dorsal root ganglion neurons is a novel effector for GABA(B) receptor activation. Neurosci Lett. 2003 Mar 6;338(3):181-4. doi: 10.1016/s0304-3940(02)01369-1. PMID: 12581826. 9: Hue B, Amat C. Activation of picrotoxin-resistant GABA receptors by GABA and related compounds induces modulation of cockroach dorsal paired median (DPM) neuron firing. J Insect Physiol. 1997 Nov;43(12):1125-1131. doi: 10.1016/s0022-1910(97)00077-2. PMID: 12770485. 10: Johnston T, Duty S. GABA(B) receptor agonists reverse akinesia following intranigral or intracerebroventricular injection in the reserpine-treated rat. Br J Pharmacol. 2003 Aug;139(8):1480-6. doi: 10.1038/sj.bjp.0705372. PMID: 12922935; PMCID: PMC1573971. 11: Jackson GL, Kuehl D. Effects of applying gamma-aminobutyric acid(B) drugs into the medial basal hypothalamus on basal luteinizing hormone concentrations and on luteinizing hormone surges in the female sheep. Biol Reprod. 2004 Feb;70(2):334-9. doi: 10.1095/biolreprod.103.021311. Epub 2003 Oct 15. PMID: 14561650. 12: Fields AM, Richards TA, Felton JA, Felton SK, Bayer EZ, Ibrahim IN, Kaye AD. Analysis of responses to valerian root extract in the feline pulmonary vascular bed. J Altern Complement Med. 2003 Dec;9(6):909-18. doi: 10.1089/107555303771952253. PMID: 14736362. 13: Carai MA, Vacca G, Serra S, Colombo G, Froestl W, Gessa GL. Suppression of GABA(B) receptor function in vivo by disulfide reducing agent, DL-dithiothreitol (DTT). Psychopharmacology (Berl). 2004 Jul;174(2):283-90. doi: 10.1007/s00213-003-1737-y. PMID: 14760512. 14: Besheer J, Lepoutre V, Hodge CW. GABA(B) receptor agonists reduce operant ethanol self-administration and enhance ethanol sedation in C57BL/6J mice. Psychopharmacology (Berl). 2004 Jul;174(3):358-66. doi: 10.1007/s00213-003-1769-3. Epub 2004 Feb 19. PMID: 14985930. 15: Piqueras L, Martinez V. Peripheral GABAB agonists stimulate gastric acid secretion in mice. Br J Pharmacol. 2004 Jul;142(6):1038-48. doi: 10.1038/sj.bjp.0705876. Epub 2004 Jun 21. PMID: 15210585; PMCID: PMC1575121. 16: Hoskison MM, Connor JA, Shuttleworth CW. GABA(B)-receptor modulation of short-term synaptic depression at an excitatory input to murine hippocampal CA3 pyramidal neurons. Neurosci Lett. 2004 Jul 15;365(1):48-53. doi: 10.1016/j.neulet.2004.04.050. PMID: 15234471. 17: Kaye AD, Hoover JM, Baber SR, Ibrahim IN, Fields AM. Analysis of gamma- aminobutyric acid-mediated responses in the pulmonary vascular bed of the cat. Anesth Analg. 2004 Sep;99(3):758-63, table of contents. doi: 10.1213/01.ANE.0000143790.39490.BD. PMID: 15333407. 18: Hoover JM, Kaye AD, Ibrahim IN, Fields AM, Richards TA. Analysis of responses to St. John's Wort in the feline pulmonary vascular bed. J Herb Pharmacother. 2004;4(3):47-62. PMID: 15829469. 19: Hoover JM, Kaye AD, Ibrahim IN, Fields AM, Richards TA. Analysis of responses to kava kava in the feline pulmonary vascular bed. J Med Food. 2006 Spring;9(1):62-71. doi: 10.1089/jmf.2006.9.62. PMID: 16579730. 20: Osawa Y, Xu D, Sternberg D, Sonett JR, D'Armiento J, Panettieri RA, Emala CW. Functional expression of the GABAB receptor in human airway smooth muscle. Am J Physiol Lung Cell Mol Physiol. 2006 Nov;291(5):L923-31. doi: 10.1152/ajplung.00185.2006. Epub 2006 Jul 7. PMID: 16829628.