PF-05175157

Name: PF-05175157
Brand: MedChemExpress
SKU: HY-12942
Rating: 5.0 (3 reviews)

Cat. No.: HY-12942 Purity: 98.10%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

PF-05175157 is broad spectrum acetyl-CoA carboxylase (ACC) inhibitor with IC₅₀s of 27.0, 33.0, 23.5 and 50.4 nM for ACC1 (human), ACC2 (human), ACC1 (rat), ACC2 (rat), respectively.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

PF-05175157 화학구조

CAS No. : 1301214-47-0

사이즈	재고	수량

무료 샘플 (0.1 - 0.2 mg)	지금 신청하기
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	해외재고보유	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	해외재고보유	Estimated Time of Arrival: December 31
Solid
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

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This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 3 publication(s) in Google Scholar

3 Publications Citing Use of MCE PF-05175157

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Biological Activity
Protocol
순도&문서
References
고객리뷰

제품 설명

PF-05175157 is broad spectrum acetyl-CoA carboxylase (ACC) inhibitor with IC₅₀s of 27.0, 33.0, 23.5 and 50.4 nM for ACC1 (human), ACC2 (human), ACC1 (rat), ACC2 (rat), respectively.

IC₅₀ & Target

IC50: 27.0 nM (ACC1 (human)), 33.0 nM (ACC2 (human)), 23.5 nM (ACC1 (rat)), 50.4 nM (ACC2 (rat))^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
Hepatocyte	EC₅₀	29.9 1 Compound: 9	Inhibition of malonyl-CoA formation in Wistar rat hepatocytes after 5 hrs by mass spectrometry Inhibition of malonyl-CoA formation in Wistar rat hepatocytes after 5 hrs by mass spectrometry	[PMID: 25423286]
Hepatocyte	EC₅₀	29.9 1 Compound: 9	Inhibition of malonyl-CoA formation in Wistar rat hepatocytes after 5 hrs by mass spectrometry Inhibition of malonyl-CoA formation in Wistar rat hepatocytes after 5 hrs by mass spectrometry	[PMID: 25423286]
Hepatocyte	EC₅₀	29.9 1 Compound: 9	Inhibition of malonyl-CoA formation in Wistar rat hepatocytes after 5 hrs by mass spectrometry Inhibition of malonyl-CoA formation in Wistar rat hepatocytes after 5 hrs by mass spectrometry	[PMID: 25423286]

In Vitro

PF-05175157 is broad spectrum acetyl-CoA carboxylase (ACC) inhibitor with IC₅₀s of 27.0±2.7, 33.0±4.1, 23.5±1.1 and 50.4±2.6 nM for ACC1 (human), ACC2 (human), ACC1 (rat) and ACC2 (rat), respectively. The in vitro metabolism of PF-05175157 (Compound 9) is evaluated in microsomes from rat, dog, and human hepatocytes. PF-05175157 is not metabolized in rat, dog, or human microsomes. PF-05175157 is also stable in human hepatocyte incubations, but is minimally metabolized by recombinant human CYP3A4 and CYP3A5. PF-05175157 inhibits formation of malonyl-CoA in a concentration-dependent manner with a potency (EC₅₀=30 nM) in rat hepatocytes consistent with its potency against rat ACC1 (24 nM)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Oral administration (3 mg/kg) to rats and dogs show bioavailability of 40% and 54%, respectively, consistent with the low microsomal clearance and good solubility at low pH. Formation of the direct product of ACC, malonyl-CoA, in the skeletal muscle and liver of lean rats is assessed 1 h following an acute oral dose of PF-05175157, showing concentration-dependent reductions in both skeletal muscle and liver malonyl-CoA. At the nadir, quadriceps and liver malonyl-CoA levels are reduced by 76% and 89%, respectively. The EC₅₀s for inhibition of quadriceps and liver malonyl-CoA are 870 and 540 nM, respectively, determined from unbind plasma concentrations of PF-05175157. Acute oral administration of PF-05175157 inhibits hepatic DNL in rats in an unbind plasma drug concentration-dependent manner. PF-05175157 inhibits up to 82% of the incorporation of [¹⁴C]acetate into [¹⁴C]lipids with an EC₅₀ of 326 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

분자량

405.49

화학식

C₂₃H₂₇N₅O₂

CAS No.

1301214-47-0

Appearance

Solid

Color

White to off-white

SMILES

O=C1CC2(CCN(C(C3=CC=C4C(NC(C)=N4)=C3)=O)CC2)CC5=C1N(C(C)C)N=C5

선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

용액&용해도

In Vitro:

DMSO : 30 mg/mL (73.98 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4662 mL	12.3308 mL	24.6615 mL
5 mM	0.4932 mL	2.4662 mL	4.9323 mL
10 mM	0.2466 mL	1.2331 mL	2.4662 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

몰농도 계산기
농도 희석 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (2.47 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (2.47 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1 mg/mL (2.47 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

순도&문서

Purity: 98.10%

Select Batch:

Data Sheet (276 KB) SDS (254 KB)

COA (247 KB) HNMR (259 KB) LCMS (101 KB)

Handling Instructions (2659 KB)

References

[1]. David A, et al. Decreasing the Rate of Metabolic Ketone Reduction in the Discovery of a Clinical Acetyl-CoA Carboxylase Inhibitor for the Treatment of Diabetes. J Med Chem. 2014 Dec 26; 57(24): 10512–10526. [Content Brief]

Cell Assay ^[1]	On the day of the study, media is aspirated and cells are treated with fresh MCM media containing DMSO vehicle or varying concentrations of PF-05175157 (Compound 9). After 5 h at 37 °C, incubation media is removed and the experiment is terminated by washing the cells with ice-cold PBS^[1]. MCE 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
Animal Administration ^[1]	Male SD rats are weighed and randomized by body weight into treatment groups consisting of vehicle, 0.25, 0.5, 1, 2, 4, 8, 15, 25, 50, and 100 mg/kg of PF-05175157 (Compound 9). Animals are orally dosed 2 h into the light cycle with their respective treatments and fed ad libitum. One hour postdose, the animals are sacrificed via CO₂ asphyxiation following by cervical dislocation. Blood for plasma exposure of PF-05175157 is collected via cardiac puncture, transferred to tubes with K₂EDTA, centrifuged at 4 °C, and the plasma transferred to a 96-well microtiter plate and stored at -20 °C. Liver and quadriceps are rapidly removed, freeze-clamped in a clamp, and subsequently stored at -80 °C^[1]. MCE 는 독립적으로 이러한 방법들의 정확성을 확인하지 않았습니다. 참고용으로만 봐주십시오.
References	[1]. David A, et al. Decreasing the Rate of Metabolic Ketone Reduction in the Discovery of a Clinical Acetyl-CoA Carboxylase Inhibitor for the Treatment of Diabetes. J Med Chem. 2014 Dec 26; 57(24): 10512–10526. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.4662 mL	12.3308 mL	24.6615 mL	61.6538 mL
	5 mM	0.4932 mL	2.4662 mL	4.9323 mL	12.3308 mL
	10 mM	0.2466 mL	1.2331 mL	2.4662 mL	6.1654 mL
	15 mM	0.1644 mL	0.8221 mL	1.6441 mL	4.1103 mL
	20 mM	0.1233 mL	0.6165 mL	1.2331 mL	3.0827 mL
	25 mM	0.0986 mL	0.4932 mL	0.9865 mL	2.4662 mL
	30 mM	0.0822 mL	0.4110 mL	0.8221 mL	2.0551 mL
	40 mM	0.0617 mL	0.3083 mL	0.6165 mL	1.5413 mL
	50 mM	0.0493 mL	0.2466 mL	0.4932 mL	1.2331 mL
	60 mM	0.0411 mL	0.2055 mL	0.4110 mL	1.0276 mL

PF-05175157 Related Classifications

Metabolic Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PF-051751571301214-47-0PF05175157PF 05175157Acetyl-CoA CarboxylaseACC, Acetyl Coenzyme A CarboxylaseInhibitorinhibitorinhibit

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PF-05175157

고객리뷰

PF-05175157 Related Antibodies

3 Publications Citing Use of MCE PF-05175157

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Protocol

순도&문서

References

고객리뷰

PF-05175157 Related Antibodies

몰농도 계산기

농도 희석 계산기

Complete Stock Solution Preparation Table

PF-05175157 Related Classifications

Keywords:

최근 본 상품:

고객리뷰

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report