Description
DHQZ 36 is a potent inhibitor of retrograde trafficking. DHQZ 36 inhibits Leishmania amazonensis infection in macrophages with an EC50 of 13.63 μM. DHQZ 36 has potent anti-parasite activity.
Product information
CAS Number: 1542098-94-1
Molecular Weight: 384.44
Formula: C21H18F2N2OS
Chemical Name: 2-(5-ethylthiophen-2-yl)-6-fluoro-3-[(4-fluorophenyl)methyl]-1,2,3,4-tetrahydroquinazolin-4-one
Smiles: CCC1=CC=C(S1)C1NC2=CC=C(F)C=C2C(=O)N1CC1C=CC(F)=CC=1
InChiKey: SVXVTSKHYHQIPJ-UHFFFAOYSA-N
InChi: InChI=1S/C21H18F2N2OS/c1-2-16-8-10-19(27-16)20-24-18-9-7-15(23)11-17(18)21(26)25(20)12-13-3-5-14(22)6-4-13/h3-11,20,24H,2,12H2,1H3
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
With increasing concentrations of DHQZ 36 there is a significant diminution in the size of parasitophorous vacuoles (LPVs), vacuole sizes are reduced by 30% at 50 μM. These parasites also cause a reduction in the number of parasites per macrophage. Significant parasite loss is observed with as low as 5 μM after treatment with DHQZ 36. Parasites are unable to recover growth when treated with DHQZ 36 at concentrations at or above 12.5 μM. DHQZ 36 causes over 40% reduction in secreted of parasite proteins. DHQZ 36 causes a reversal in Leishmania induced suppression of IL-6 release by infected cells after LPS activation.
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