MedKoo Cat#: 574347 | Name: DS1

Description:

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

DS1 is a small molecule that selectively enhances the activity of extrasynaptic GABAA receptors containing the δ-subunit, without significantly affecting synaptic GABA<sub>A</sub> receptors. It acts as a positive allosteric modulator, potentiating tonic inhibitory currents in the brain and offering potential therapeutic utility in disorders involving hyperexcitability, such as epilepsy or anxiety. DS1 exhibits high selectivity and potency, making it a valuable pharmacological tool for studying the role of δ-containing GABAA receptors in CNS function.

Chemical Structure

DS1
DS1
CAS#372497-52-4

Theoretical Analysis

MedKoo Cat#: 574347

Name: DS1

CAS#: 372497-52-4

Chemical Formula: C18H10Br2ClN3OS

Exact Mass: 508.8600

Molecular Weight: 511.62

Elemental Analysis: C, 42.26; H, 1.97; Br, 31.24; Cl, 6.93; N, 8.21; O, 3.13; S, 6.27

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Synonym
DS1; DS 1; DS-1
IUPAC/Chemical Name
4-Chloro-N-[6,8-dibromo-2-(2-thienyl)imidazo[1,2-a]pyridin-3-yl]benzamide;
InChi Key
MEWSBNIVOLYKGU-UHFFFAOYSA-N
InChi Code
InChI=1S/C18H10Br2ClN3OS/c19-11-8-13(20)16-22-15(14-2-1-7-26-14)17(24(16)9-11)23-18(25)10-3-5-12(21)6-4-10/h1-9H,(H,23,25)
SMILES Code
O=C(NC1=C(C2=CC=CS2)N=C3C(Br)=CC(Br)=CN31)C4=CC=C(Cl)C=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
>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
Biological target:
DS1 is a GABAA receptor agonist which can stimulate gonadotropin subunit gene expression in mouse.
In vitro activity:
DS-1 significantly inhibited the proliferation of lung cancer cells compared to the control. The aggressive behavior of cancer cells, including migration and invasion, was significantly reduced by DS-1. DS-1 suppressed lung cancer metastasis via suppressing EMT, integrin β1 expression and FAK-related signaling. Reference: Anticancer Res. 2021 Jun;41(6):2913-2923. https://pubmed.ncbi.nlm.nih.gov/34083282/
In vivo activity:
This study examined the effect of DS1, a GABAA α4β3δ receptor agonist, on a strain of mouse hypothalamic immortalized GnRH neuronal cells, the GT1-7 cell line. The current observations suggest that DS1 exerts its stimulatory effect on the intracellular signal transduction system via GABAA α4β3δ receptors in GnRH-producing neurons. Stimulation with DS1 increased the expression of GnRH receptor but decreased the basal expression of GnRH mRNA. Reference: Endocrine. 2015 May;49(1):222-30. https://pubmed.ncbi.nlm.nih.gov/25355308/

Preparing Stock Solutions

The following data is based on the product molecular weight 511.62 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. Putri HE, Sritularak B, Chanvorachote P. DS-1 Inhibits Migration and Invasion of Non-small-cell Lung Cancer Cells Through Suppression of Epithelial to Mesenchymal Transition and Integrin β1/FAK Signaling. Anticancer Res. 2021 Jun;41(6):2913-2923. doi: 10.21873/anticanres.15073. PMID: 34083282. 2. 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. 3. Sukhbaatar U, Mijiddorj T, Oride A, Kanasaki H. Stimulation of δ subunit-containing GABAA receptor by DS1 increases GnRH receptor expression but reduces GnRH mRNA expression in GnRH-producing GT1-7 cells. Endocrine. 2015 May;49(1):222-30. doi: 10.1007/s12020-014-0464-y. Epub 2014 Oct 30. PMID: 25355308.
In vitro protocol:
1. Putri HE, Sritularak B, Chanvorachote P. DS-1 Inhibits Migration and Invasion of Non-small-cell Lung Cancer Cells Through Suppression of Epithelial to Mesenchymal Transition and Integrin β1/FAK Signaling. Anticancer Res. 2021 Jun;41(6):2913-2923. doi: 10.21873/anticanres.15073. PMID: 34083282. 2. 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.
In vivo protocol:
1. Sukhbaatar U, Mijiddorj T, Oride A, Kanasaki H. Stimulation of δ subunit-containing GABAA receptor by DS1 increases GnRH receptor expression but reduces GnRH mRNA expression in GnRH-producing GT1-7 cells. Endocrine. 2015 May;49(1):222-30. doi: 10.1007/s12020-014-0464-y. Epub 2014 Oct 30. PMID: 25355308.
Mijiddorj, T., et al.: Biol. Reprod., 92, 45/1-45/8 (2015)