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  3. LASSBio-1736

LASSBio-1736 is a Cysteine protease inhibitor and antimalarial agent. LASSBio-1736 targets the promastigote form of Leishmania major. LASSBio-1736 can be used in the research of leishmaniasis.

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

LASSBio-1736

LASSBio-1736 Chemical Structure

CAS No. : 1554691-37-0

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Description

LASSBio-1736 is a Cysteine protease inhibitor and antimalarial agent. LASSBio-1736 targets the promastigote form of Leishmania major. LASSBio-1736 can be used in the research of leishmaniasis[1][2][3].

IC50 & Target[1]

Leishmania

 

In Vitro

LASSBio-1736 (up to 100 μM) potently inhibits the growth of Leishmania major promastigotes; additionally, it shows no cytotoxicity against J774 murine macrophages at concentrations up to 100 μM[1].
LASSBio-1736 can penetrate the simulated blood-brain barrier, with a permeability coefficient of 10.63 × 10−6 cm s-1[2].
LASSBio-1736 (5 μM; 0-240 min) exhibits high stability in rat plasma, with a half-life of 28.9 h and only 7.30% metabolic conversion within 240 minutes[2].
LASSBio-1736 potently inhibits the growth of Leishmania major promastigotes with an IC50 of 0.4 μg/mL, and exhibits no cytotoxicity against J774 mouse macrophages[3].

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

Parmacokinetics
Species Dose Route T1/2 Vd CLtotal MRT Cmax Tmax AUC0-∞ Vdss
Rat[1] 3.2 mg/kg i.v. / / 49.3 mL/h/kg 23.6 h / / 67 μg·h/mL 1.16 L/kg
Rat[1] 12.6 mg/kg p.o. 28.6 h 1.47 L/kg 49.7 mL/h/kg 30.06 h 1.08 μg/mL 5.6 h / /
Rat[1] 12.6 mg/kg i.p. 26 h 1.8 L/kg 58 mL/h/kg 30.4 h 2.5 μg/mL 6.5 h / /
In Vivo

LASSBio-1736 (30 μmol/kg; intraperitoneal injection; once daily for 28 consecutive days) exhibits significant antileishmanial efficacy in a BALB/c mouse model of cutaneous leishmaniasis, and reduces the number of amastigotes in target tissues[1].

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

Animal Model: BALB/c (male)[1]
Dosage: 30 μmol/kg
Administration: i.p.; daily; 28 days
Result: Caused a significant decrease in the number of Leishmania amazonensis amastigotes in the mouse ear dermis and lymph nodes compared to glucantime (administered at the same dose and schedule).
Molecular Weight

419.19

Formula

C16H11Cl2F3N4O2

CAS No.
SMILES

O=C(NNC(C1=CC=C(Cl)C=C1Cl)=O)N/N=C/C2=CC=C(C(F)(F)F)C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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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.

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Product Name:
LASSBio-1736
Cat. No.:
HY-184205
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