PS10 - ≥99% , CAS No.1564265-82-2

CAS: 1564265-82-2 Cat. No.: P647045 분자식: C₁₄H₁₃NO₆S 분자량: 323.32

GRADE & PURITY ≥99%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

개요

PS10 is a novel, potent and ATP-competitive pan- PDK inhibitor, inhibits all PDK isoforms with IC 50 of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM for PDK2, PDK4, PDK1, and PDK3, respectively. PS10 shows high affinity for PDK2 ( K d = 239 nM) than for Hsp90 (K d = 47 μM) PS10 improves glucose tolerance, stimulates myocardial carbohydrate oxidation in diet-induced obesity. PS10 has the potential for the investigation of diabetic cardiomyopathy .PDK: pyruvate dehydrogenase kinase

In Vitro

PS10 shows a higher affinity of PS10 for PDK2 (K d = 239 nM) than for Hsp90 (K d = 47,000 nM). PS10 is less potent than cycloheximide in HeLa cells, it shows an IC 50 value of 284 μM for the growth inhibition and PS10 has low toxicity in cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PS10 (Intraperitoneal injection; 70 mg/kg; single dose) treatment lead to 11- and 23-fold higher PDC activity in heart and liver, respectively. Meanwhile, there results in a 1.4-fold enhancement of PDC activity in kidneys compared with vehicle-group . PS10 (Intraperitoneal injection; 70 mg/kg; 3 days) treatment results that thePDC activity profiles and the phospho-E1α subunit level is similar to the single-dose. Notably, the three-day treatment attenuates the enhancement of PDK activity in heart . PS10 (intraperitoneal injection; 70 mg/kg; 4 weeks) is treated in mice and subjected to a glucose tolerance test. when challenged with 1.5 g/kg glucose, the plasma glucose level in the vehicle-treated control is at 200 mg/dl at 0 min, peaks at 482 mg/dl at 30 min, and reduces to 210 mg/dl at 120 min. In PS10-treated DIO mice, the glucose level at 168 mg/dl at 0 min is lower than that in vehicle-treated animals, reachs 312 mg/dl at 30 min, and returns to 163 mg/dl at 120 min . PS10 (intraperitoneal injection; 70 mg/kg) and DCA both stimulates flux through PDC as measured by the appearance of hyperpolarized [ 13 C]bicarbonate. It shows similar glucose tolerance response to glucose challenge restores PDC activity in the DIO mouse hearts. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57BL/6J male mice at 6 to 8 weeks oldDosage: 70 mg/kg/day Administration: Intraperitoneal injection Result: Improved glucose tolerance in the intact animal.

Form:Solid

IC50& Target:IC50: 0.8 μM (PDK2),0.76 μM (PDK4),2.1 μM (PDK3),21.3 μM (PDK1)

Specifications

사양 및 순도

≥99%

생화학 및 생리적 메커니즘

PS10 is a novel, potent and ATP-competitive pan- PDK inhibitor, inhibits all PDK isoforms with IC 50 of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM for PDK2, PDK4, PDK1, and PDK3, respectively. PS10 shows high affinity for PDK2 ( K d = 239 nM) than for Hsp90 (K d

보관 조건

Store at -20°C

배송

Ice chest + Ice pads

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작업 유형

INHIBITOR

순수함

≥99%

이름과 식별자

• 분자량: 323.32

화학 및 물리적 특성

• 용해성: DMSO : 62.5 mg/mL (193.31 mM; Need ultrasonic)

자주 묻는 질문

What is the purity of this product?

This product is supplied at ≥99% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How should this product be stored?

Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1564265-82-2, the molecular formula is C14H13NO6S, and the molecular weight is 323.32 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.