2. Metabolic Enzyme/Protease
  3. MMP
  4. BI-4394

BI-4394  (Synonyms: MMP13-IN-3)

Cat. No.: HY-124029 Purity: 99.91%
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BI-4394 (MMP13-IN-3) is a potent, selective, and orally active MMP-13 inhibitor (IC50=1 nM) for the potential treatment of osteoarthritis. BI-4394 is >1000 selective over other MMPs.

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

BI-4394 Chemical Structure

BI-4394 Chemical Structure

CAS No. : 1222173-37-6

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Solid + Solvent
10 mM * 1 mL in DMSO
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 USD 330 In-stock
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10 mM * 1 mL in DMSO USD 330 In-stock
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10 mg USD 480 In-stock
50 mg USD 1450 In-stock
100 mg USD 2250 In-stock
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Based on 1 publication(s) in Google Scholar

BI-4394 Related Antibodies

Top Publications Citing Use of Products

View All MMP Isoform Specific Products:

View All Isoforms
MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8

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Description

BI-4394 (MMP13-IN-3) is a potent, selective, and orally active MMP-13 inhibitor (IC50=1 nM[1]) for the potential treatment of osteoarthritis[2]. BI-4394 is >1000 selective over other MMPs[1].

IC50 & Target[1]

MMP-13

1 nM (IC50)

MMP-14

8.3 μM (IC50)

MMP-9

8.9 μM (IC50)

MMP-10

16 μM (IC50)

MMP-2

18 μM (IC50)

In Vitro

BI-4394 (Compound 15) is potent in a full-length MMP-13 collagen degradation assay (11 nM) and is able to inhibit degradation of bovine nasal cartilage with an IC50 of 31 nM. BI-4394 inhibits MMP-2, MMP-9, MMP-10 and MMP-14 with IC50s of 18, 8.9, 16 and 8.3 μM, respectively[1].

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

BI-4394 Related Antibodies
In Vivo

When dosed orally at 10 mg/kg or i.v. 1 mg/kg, BI-4394 (Compound 15) reaches micromolar plasma levels (AUC=1109±64 nM h/mL), displays modest clearance (CL=34 mL/min/kg), and shows acceptable bioavailability (39%). The Vss is quite low at 0.26 mL/mi/kg rat pharmacokinetic profile. BI-4394 has short terminal elimination half-life (t1/2=0.47 h for rat (1 mg/kg, i.v.) and rat (10 mg/kg, orally), respectively)[1].

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

Animal Model: Srapgue Dally Rats[1]
Dosage: 10 mg/kg (oral gavage); 1 mg/kg (i.v.)
Administration: Dosed orally (10 mg/kg); i.v. (1 mg/kg)(Pharmacokinetic Analysis)
Result: T1/2=0.47 h for rat (1 mg/kg, i.v.) and rat (10 mg/kg, orally) , respectively.
Molecular Weight

446.46

Formula

C24H22N4O5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C(N1)=CC2=C1C=CC(C3=CC(C(NCC4=CC=C(C(O)=O)C=C4)=O)=NN3C)=C2)OCC
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 (223.98 mM; ultrasonic and warming and heat to 60°C; 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 2.2398 mL 11.1992 mL 22.3984 mL
5 mM 0.4480 mL 2.2398 mL 4.4797 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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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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C2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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g

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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. 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 2.2398 mL 11.1992 mL 22.3984 mL 55.9961 mL
5 mM 0.4480 mL 2.2398 mL 4.4797 mL 11.1992 mL
10 mM 0.2240 mL 1.1199 mL 2.2398 mL 5.5996 mL
15 mM 0.1493 mL 0.7466 mL 1.4932 mL 3.7331 mL
20 mM 0.1120 mL 0.5600 mL 1.1199 mL 2.7998 mL
25 mM 0.0896 mL 0.4480 mL 0.8959 mL 2.2398 mL
30 mM 0.0747 mL 0.3733 mL 0.7466 mL 1.8665 mL
40 mM 0.0560 mL 0.2800 mL 0.5600 mL 1.3999 mL
50 mM 0.0448 mL 0.2240 mL 0.4480 mL 1.1199 mL
60 mM 0.0373 mL 0.1867 mL 0.3733 mL 0.9333 mL
80 mM 0.0280 mL 0.1400 mL 0.2800 mL 0.7000 mL
100 mM 0.0224 mL 0.1120 mL 0.2240 mL 0.5600 mL
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BI-4394 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:

BI-43941222173-37-6MMP13-IN-3BI4394BI 4394MMPMatrix metalloproteinasesMMP-13osteoarthritisInhibitorinhibitorinhibit

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