2. Membrane Transporter/Ion Channel
  3. Sodium Channel
  4. PF-06649298

PF-06649298 is a sodium-coupled citrate transporter (NaCT or SLC13A5) inhibitor. PF-06649298 specifically interacts with NaCT with an IC50 value of 16.2 μM to inhibits the transport of citrate in human hepatocytes. PF-06649298 can be used for the research of regulating glucose metabolism and lipid metabolism.

For research use only. We do not sell to patients.

PF-06649298 Chemical Structure

PF-06649298 Chemical Structure

CAS No. : 1854061-16-7

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 495 In-stock
Solution
10 mM * 1 mL in DMSO USD 495 In-stock
Solid
5 mg USD 450 In-stock
10 mg USD 800 In-stock
25 mg USD 1650 In-stock
50 mg USD 2550 In-stock
100 mg USD 3800 In-stock
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Based on 1 publication(s) in Google Scholar

PF-06649298 Related Antibodies

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Description

PF-06649298 is a sodium-coupled citrate transporter (NaCT or SLC13A5) inhibitor. PF-06649298 specifically interacts with NaCT with an IC50 value of 16.2 μM to inhibits the transport of citrate in human hepatocytes. PF-06649298 can be used for the research of regulating glucose metabolism and lipid metabolism[1][2].

IC50 & Target

IC50: 408 nM (citrate uptake in HEKNaCT), 16.2 μM (citrate uptake in Human Heps), 4.5 μM (citrate uptake in Mouse Heps), ＞100 μM (citrate uptake in HEKNaCD1), ＞100 μM (citrate uptake in HEKNaCD3)[1][2]
In Vitro

PF-06649298 (0-100 μM; 30 min) inhibits citrate uptaken in cells[1].

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

PF-06649298 Related Antibodies

Cell Viability Assay[1]

Cell Line: HEK-293 cells expressing NaCT, NaDC1 or NaDC3, human hepatocytes and mouse epatocytes
Concentration: 0-100 μM
Incubation Time: 30 min
Result: Showed a selectivity for NaCT over the dicarboxylate transporters NaDC1 and NaDC3. Inhibited citrate uptake in HEK-293 cells expressing NaCT, NaDC1 or NaDC3, human hepatocytes and mouse epatocytes with IC50s of 408 nM, ＞100 μM, ＞100 μM, 16.2 μM and 4.5 μM, respectively.
In Vivo

PF-06649298 (250 mg/kg; p.o. twice a day; for 21 days) reverses glucose intolerance of high fat diet (HFD) mice[2].

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

Animal Model: Mice with high fat diet (HFD) administration[2]
Dosage: 250 mg/kg
Administration: Oral gavage; 250mg/kg twice a day; for 21 days
Result: Decreased plasma glucose, hepatic triglycerides, diacylglycerides, and acyl-carnitines concentration of livers in HFD mice. Totally reversed glucose intolerance of HFD mice.
Molecular Weight

294.34

Formula

C16H22O5
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(O)[C@@](O)(CCC1=CC=C(C(C)(C)C)C=C1)CC(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (339.74 mM; Need ultrasonic; 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 3.3974 mL 16.9872 mL 33.9743 mL
5 mM 0.6795 mL 3.3974 mL 6.7949 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo Dissolution Calculator
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Purity & Documentation
References

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3974 mL 16.9872 mL 33.9743 mL 84.9358 mL
5 mM 0.6795 mL 3.3974 mL 6.7949 mL 16.9872 mL
10 mM 0.3397 mL 1.6987 mL 3.3974 mL 8.4936 mL
15 mM 0.2265 mL 1.1325 mL 2.2650 mL 5.6624 mL
20 mM 0.1699 mL 0.8494 mL 1.6987 mL 4.2468 mL
25 mM 0.1359 mL 0.6795 mL 1.3590 mL 3.3974 mL
30 mM 0.1132 mL 0.5662 mL 1.1325 mL 2.8312 mL
40 mM 0.0849 mL 0.4247 mL 0.8494 mL 2.1234 mL
50 mM 0.0679 mL 0.3397 mL 0.6795 mL 1.6987 mL
60 mM 0.0566 mL 0.2831 mL 0.5662 mL 1.4156 mL
80 mM 0.0425 mL 0.2123 mL 0.4247 mL 1.0617 mL
100 mM 0.0340 mL 0.1699 mL 0.3397 mL 0.8494 mL
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PF-06649298 Related Classifications

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-066492981854061-16-7PF06649298PF 06649298Sodium ChannelNa channelsNa+ channelscitrateglucose intoleranceHFDDIOdiacylglyceridehepatic triglycerideacyl-carnitineInhibitorinhibitorinhibit

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