SRT3025 HCl
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MedKoo CAT#: 533066

CAS#: 2070015-26-6 (HCl)

Description: SRT3025 is a Novel Sirtuin1 Activator, Down-Regulating Sclerostin and Rescuing Ovariectomy-Induced Bone Loss.


Chemical Structure

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SRT3025 HCl
CAS# 2070015-26-6 (HCl)

Theoretical Analysis

MedKoo Cat#: 533066
Name: SRT3025 HCl
CAS#: 2070015-26-6 (HCl)
Chemical Formula: C31H32ClN5O2S2
Exact Mass: 0.00
Molecular Weight: 606.200
Elemental Analysis: C, 61.42; H, 5.32; Cl, 5.85; N, 11.55; O, 5.28; S, 10.58

Price and Availability

Size Price Availability Quantity
5mg USD 150 Ready to ship
10mg USD 250 Ready to ship
25mg USD 450 Ready to ship
50mg USD 750 Ready to ship
100mg USD 1250 Ready to ship
200mg USD 1950 Ready to ship
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Related CAS #: 1231952-55-8 (free base)   2070015-26-6 (HCl)    

Synonym: SRT3025; SRT-3025; SRT 3025; SRT3025 HCl; SRT3025 hydrochloride

IUPAC/Chemical Name: 5-(3-Methoxypropyl)-2-phenyl-N-[2-[6-(1-pyrrolidinylmethyl)thiazolo[5,4-b]pyridin-2-yl]phenyl]-4-thiazolecarboxamide hydrochloride

InChi Key: LGRBDTOIPNDWMN-UHFFFAOYSA-N

InChi Code: InChI=1S/C31H31N5O2S2.ClH/c1-38-17-9-14-26-27(35-29(39-26)22-10-3-2-4-11-22)28(37)33-24-13-6-5-12-23(24)30-34-25-18-21(19-32-31(25)40-30)20-36-15-7-8-16-36;/h2-6,10-13,18-19H,7-9,14-17,20H2,1H3,(H,33,37);1H

SMILES Code: O=C(C1=C(CCCOC)SC(C2=CC=CC=C2)=N1)NC3=CC=CC=C3C4=NC5=CC(CN6CCCC6)=CN=C5S4.[H]Cl

Appearance: Fluffy yellow 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:

Biological target: Sirtuin modulator 1 is a modulator of SIRTl, a homolog of SIRT3, with EC1.5 of < 1 μM, extracted from patent WO 2010071853 A1, Compound No.4.
In vitro activity: To investigate if the effects of Sirt1 on the marrow adipocyte phenotype can be extended to human BM-MSCs, SRT3025 was administered to primary human femoral BM-MSCs. Strikingly, SRT3025-treated human BM-MSCs had increased mRNA expression of PGC1α (Figure 6A) accompanied by elevated PGC1α protein level (Figure 6B), suggesting that Sirt1 activates PGC1α in human femoral BM-MSCs. Reference: Front Endocrinol (Lausanne). 2019 Feb 28;10:126. https://pubmed.ncbi.nlm.nih.gov/30873124/
In vivo activity: Diabetic mice that had received SRT3025 had improved glycaemic control as manifested by lower HbA1c, fasting and non-fasting blood glucose concentrations (Fig. 1A,B). Fasting plasma insulin concentrations were below the limits of detection by ELISA in animals that had received STZ regardless of their assignment to receive SRT3025 or not and while detectable but very low in the non-fasting state, concentrations did not vary according to treatment assignment (Fig. 2A). Plasma glucagon was markedly elevated in untreated diabetic mice but was substantially reduced with SRT3025 (Fig. 2B). Reference: Sci Rep. 2018 Sep 18;8(1):13972. https://pubmed.ncbi.nlm.nih.gov/30228292/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 56.3 92.79
Ethanol 5.0 8.25

Preparing Stock Solutions

The following data is based on the product molecular weight 606.20 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. Artsi H, Gurt I, El-Haj M, Müller R, Kuhn GA, Ben Shalom G, Cohen-Kfir E, Abramowitz E, Kandel L, Safran O, Dresner-Pollak R. Sirt1 Promotes a Thermogenic Gene Program in Bone Marrow Adipocytes: From Mice to (Wo)Men. Front Endocrinol (Lausanne). 2019 Feb 28;10:126. doi: 10.3389/fendo.2019.00126. PMID: 30873124; PMCID: PMC6403178. 2. Zhang Y, Thai K, Jin T, Woo M, Gilbert RE. SIRT1 activation attenuates α cell hyperplasia, hyperglucagonaemia and hyperglycaemia in STZ-diabetic mice. Sci Rep. 2018 Sep 18;8(1):13972. doi: 10.1038/s41598-018-32351-z. PMID: 30228292; PMCID: PMC6143559. 3. Zhang QS, Deater M, Schubert K, Marquez-Loza L, Pelz C, Sinclair DA, Grompe M. The Sirt1 activator SRT3025 expands hematopoietic stem and progenitor cells and improves hematopoiesis in Fanconi anemia mice. Stem Cell Res. 2015 Jul;15(1):130-40. doi: 10.1016/j.scr.2015.05.007. Epub 2015 May 22. PMID: 26046330; PMCID: PMC4516677.
In vitro protocol: 1. Artsi H, Gurt I, El-Haj M, Müller R, Kuhn GA, Ben Shalom G, Cohen-Kfir E, Abramowitz E, Kandel L, Safran O, Dresner-Pollak R. Sirt1 Promotes a Thermogenic Gene Program in Bone Marrow Adipocytes: From Mice to (Wo)Men. Front Endocrinol (Lausanne). 2019 Feb 28;10:126. doi: 10.3389/fendo.2019.00126. PMID: 30873124; PMCID: PMC6403178.
In vivo protocol: 1. Zhang Y, Thai K, Jin T, Woo M, Gilbert RE. SIRT1 activation attenuates α cell hyperplasia, hyperglucagonaemia and hyperglycaemia in STZ-diabetic mice. Sci Rep. 2018 Sep 18;8(1):13972. doi: 10.1038/s41598-018-32351-z. PMID: 30228292; PMCID: PMC6143559. 2. Zhang QS, Deater M, Schubert K, Marquez-Loza L, Pelz C, Sinclair DA, Grompe M. The Sirt1 activator SRT3025 expands hematopoietic stem and progenitor cells and improves hematopoiesis in Fanconi anemia mice. Stem Cell Res. 2015 Jul;15(1):130-40. doi: 10.1016/j.scr.2015.05.007. Epub 2015 May 22. PMID: 26046330; PMCID: PMC4516677.

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1. Artsi H, Gurt I, El-Haj M, Müller R, Kuhn GA, Ben Shalom G, Cohen-Kfir E, Abramowitz E, Kandel L, Safran O, Dresner-Pollak R. Sirt1 Promotes a Thermogenic Gene Program in Bone Marrow Adipocytes: From Mice to (Wo)Men. Front Endocrinol (Lausanne). 2019 Feb 28;10:126. doi: 10.3389/fendo.2019.00126. PMID: 30873124; PMCID: PMC6403178.
2. Zhang Y, Thai K, Jin T, Woo M, Gilbert RE. SIRT1 activation attenuates α cell hyperplasia, hyperglucagonaemia and hyperglycaemia in STZ-diabetic mice. Sci Rep. 2018 Sep 18;8(1):13972. doi: 10.1038/s41598-018-32351-z. PMID: 30228292; PMCID: PMC6143559.
3. Zhang QS, Deater M, Schubert K, Marquez-Loza L, Pelz C, Sinclair DA, Grompe M. The Sirt1 activator SRT3025 expands hematopoietic stem and progenitor cells and improves hematopoiesis in Fanconi anemia mice. Stem Cell Res. 2015 Jul;15(1):130-40. doi: 10.1016/j.scr.2015.05.007. Epub 2015 May 22. PMID: 26046330; PMCID: PMC4516677.