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SRT1720 hydrochloride

SKU: orb1305522

Description

SRT1720 HCl is a potent and selective SIRT1 activator (EC1.5 = 0.16 µM), demonstrating significantly lower activity against SIRT2 and SIRT3. This small molecule is widely used in research to study sirtuin biology, metabolic regulation, and aging-related pathways in both cellular and animal models.

Research Area

Epigenetics & Chromatin, Molecular Biology

Images & Validation

Key Properties

CAS Number1001645-58-4
MW506.22
Purity99.59%
FormulaC25H24ClN7OS
SMILESCl.O=C(Nc1ccccc1-c1cn2c(CN3CCNCC3)csc2n1)c1cnc2ccccc2n1
TargetSirtuin
SolubilityEthanol:< 1 mg/mL (insoluble or slightly soluble);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:11.3 mg/mL (22.32 mM)

Bioactivity

Target IC50
SIRT1:0.16 μM(EC1.5, cell free)
In Vivo
SRT1720 exhibited a pharmacokinetic profile suitable for in vivo evaluation in both mouse (bioavailability = 50%, terminal t1/2 = ~5 h, Area Under the Curve (AUC) = 7,892 ng h/ml/) and rat (bioavailability = 25%, terminal t1/2 = ~8.4 h, AUC = 3,714 ng/h/ml). In DIO mice, fasting blood glucose levels are elevated (120–150 mg dl 1 range) after being placed on a high-fat diet. Administration of SRT1720 reduced fed glucose levels after 1 week of treatment with further reduction after 3 weeks of treatment that continued through 10 weeks of dosing. Glucose excursion during an intraperitoneal glucose tolerance test was also significantly reduced in the SRT1720 group, and comparable to rosiglitazone, a PPARγ activator that has been used to treat type 2 diabetes . SRT1720 attenuated stress-induced premature cellular senescence and protected against emphysema induced by cigarette smoke and elastase in mice . In animal tumour model studies, SRT1720 inhibited MM tumour growth. SRT1720 enhanced the cytotoxic activity of bortezomib or dexamethasone .
In Vitro
SRT1720 is an activator of SIRT1 (EC1.5 = 0.16 μM and maximum activation = 781%). SRT1720 is selective for activation of SIRT1 versus the closest sirtuin homologues, SIRT2 and SIRT3 (SIRT2: EC1.5 = 37 μM; SIRT3: EC1.5 > 300 μM) .
Cell Research
Cell viability was assessed with a colorimetric assay using MTT as described previously. Apoptosis assay was quantified using Annexin V-FITC/Propidium iodide (PI) apoptosis detection kit, as per manufacturer's instructions, followed by analysis on FACS Calibur .
Animal Research
Sirtinol (2 mg/kg) was administered by peritoneal injection, whereas SRT1720 (100 mg/kg) was administered through oral gavage 1 hour prior to CS exposure daily for 3 days. In a separate experiment, SRT1720 (25, 50, and 100 mg/kg) or PHA-408 (50 mg/kg) was dissolved in 0.5% carboxymethylcellulose containing 0.025% Tween 20 and injected via oral gavage into the conscious mice 24 hours prior to elastase administration, which was repeated daily (5 days per week) until 21 days after elastase administration. To study the therapeutic effect on emphysema, SRT1720 (100 mg/kg) was orally administered daily for 2 weeks after the development of elastase-induced emphysema .

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

SRT 1720 Hydrochloride, SRT1720 HCl, SRT1720 hydrochloride, SRT1720 Hydrochloride, SRT-1720 Hydrochloride, SRT-1720 hydrochloride, SIRT1

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Key Properties

No computed properties available.

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SRT1720 hydrochloride (orb1305522)

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% DMSO +
%+
% Tween 80 +
%

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5 mg
$ 200.00
25 mg
$ 400.00
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