2. Membrane Transporter/Ion Channel Metabolic Enzyme/Protease
  3. Potassium Channel Cytochrome P450
  4. ML252

ML252 is a selective inhibitor of KCNQ2 (Kv7.2) channel with an IC50s of 69 nM, 2.92 μM, 0.12 μM and 0.20 μM for KCNQ2, KCNQ1 (Kv7.1), KCNQ2/Q3 and KCNQ4, respectively. ML252 also inhibits Cytochrome P450 with IC50s of 6.1 nM (CYP1A2), 18.9 nM (CYP2C9), 3.9 nM (CYP3A4), 19.9 nM (CYP2D6), respectively. ML252 shows highly brain penetrant .

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ML252 Chemical Structure

ML252 Chemical Structure

CAS No. : 1392494-64-2

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10 mg USD 355 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of ML252:

ML252 Related Antibodies

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View All Cytochrome P450 Isoform Specific Products:

View All Isoforms
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

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  • Purity & Documentation

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  • Customer Review

Description

ML252 is a selective inhibitor of KCNQ2 (Kv7.2) channel with an IC50s of 69 nM, 2.92 μM, 0.12 μM and 0.20 μM for KCNQ2, KCNQ1 (Kv7.1), KCNQ2/Q3 and KCNQ4, respectively. ML252 also inhibits Cytochrome P450 with IC50s of 6.1 nM (CYP1A2), 18.9 nM (CYP2C9), 3.9 nM (CYP3A4), 19.9 nM (CYP2D6), respectively. ML252 shows highly brain penetrant [1][2].

IC50 & Target[1][2]

KCNQ2

69 nM (IC50)

KCNQ1

2.92 μM (IC50)

KCNQ2/Q3

0.12 μM (IC50)

KCNQ4

0.20 μM (IC50)

CYP1A2

6.1 μM (IC50)

CYP2C9

18.9 μM (IC50)

CYP2D6

19.9 μM (IC50)

CYP3A4

3.9 μM (IC50)

In Vitro

ML252 (1 μM; 0-48 h) shows an intrinsic clearance and subsequent predicted hepativ clearance of 1720 mL/min/kd and 67.3 mL/min/kg, respectively, in rat hepatic microsomes[1].
ML252 (0.1-10 μM) inhibits the current of KCNQ2 at 0.3 μM, and completely inhibits the current at 1 μM in CHO-KCNQ2 cell line[1].
ML252 (30 μM; 48 h) has no acute toxicity to CHO cells[1].

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

ML252 Related Antibodies
In Vivo

ML252 has the metabolic stability unsuitable for oral administration[2].
ML252 (10 mg/kg, 3 mg/mL; ip; single dose; measured at 1 hr after) shows a highly brain penetrant with a B:P ratio of 1.9 and absolute brain levels of 672 nM in rat model[1].

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

308.42

Formula

C20H24N2O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC=CC=C1N2CCCC2)[C@H](C3=CC=CC=C3)CC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (324.23 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 3.2423 mL 16.2117 mL 32.4233 mL
5 mM 0.6485 mL 3.2423 mL 6.4847 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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
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 (protect from light, stored under nitrogen). 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 3.2423 mL 16.2117 mL 32.4233 mL 81.0583 mL
5 mM 0.6485 mL 3.2423 mL 6.4847 mL 16.2117 mL
10 mM 0.3242 mL 1.6212 mL 3.2423 mL 8.1058 mL
15 mM 0.2162 mL 1.0808 mL 2.1616 mL 5.4039 mL
20 mM 0.1621 mL 0.8106 mL 1.6212 mL 4.0529 mL
25 mM 0.1297 mL 0.6485 mL 1.2969 mL 3.2423 mL
30 mM 0.1081 mL 0.5404 mL 1.0808 mL 2.7019 mL
40 mM 0.0811 mL 0.4053 mL 0.8106 mL 2.0265 mL
50 mM 0.0648 mL 0.3242 mL 0.6485 mL 1.6212 mL
60 mM 0.0540 mL 0.2702 mL 0.5404 mL 1.3510 mL
80 mM 0.0405 mL 0.2026 mL 0.4053 mL 1.0132 mL
100 mM 0.0324 mL 0.1621 mL 0.3242 mL 0.8106 mL
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ML252 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:

ML2521392494-64-2ML 252ML-252Potassium ChannelCytochrome P450KcsACYPsKCNQ2Kv7.2KCNQ1Kv7.1KCNQ2/Q3KCNQ4CYP1A2CYP2C9CYP3A4CYP2D6Inhibitorinhibitorinhibit

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