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Art. -Nr.: HY-184205

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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.

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CAS. Nr.: 1554691-37-0
Formel: C₁₆H₁₁Cl₂F₃N₄O₂
Molecular Weight:419.19

Speicherung:

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

LASSBio-1736 Chemical Structure

CAS. Nr.: 1554691-37-0

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Preis

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

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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	T_1/2	V_d	CL_total	MRT	C_max	T_max	AUC_0-∞	V_dss
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).

Chemical Information

CAS. Nr. 1554691-37-0
Molecular Weight 419.19
Formel C₁₆H₁₁Cl₂F₃N₄O₂
SMILES

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

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Moraes BS, et al. Leishmanicidal candidate LASSBio-1736, a cysteine protease inhibitor with favorable pharmacokinetics: low clearance and good distribution. Xenobiotica. 2018 Dec;48(12):1258-1267. [Content Brief]

[2]. de Queiroz AC, et al. Pre-clinical evaluation of LASSBio-1491: From in vitro pharmacokinetic study to in vivo leishmanicidal activity. PLoS One. 2022 Jun 6;17(6):e0269447. [Content Brief]

[3]. Moraes BKS, et al. Simple HPLC-UV for the quantification of a new leishmanicidal candidate (E)-1-4(trifluoromethyl) benzylidene)-5-(2-4-dichlorozoyl) carbonylhydrazine (LASSBio-1736) in rat plasma for pharmacokinetics assessment. Biomed Chromatogr. 2016 Jul;30(7):1029-1035. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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LASSBio-1736

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