≥98% for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
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Storage & shipping
Store at -20°C Ships Ice chest + Ice pads Check lot-specific COA for exact specifications.
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Quality documents
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
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Literature proof
Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Panoramica
GSK3494245 (DDD01305143) is a potent, orally active, and selective inhibitor of the chymotrypsin-like activity of the parasite proteasome binding in a site sandwiched between the β4 and β5 subunits ( IC 50 =0.16 μM for WT L. donovani proteasomes). GSK3494245 moderately inhibits chymotrypsin-like activity of human proteasome (IC 50 : purified 26S=13 µM; enriched THP-1 extracts IC 50 =40µM). GSK3494245 exhibits attractive biological and biosafety properties.
In Vitro
GSK3494245 shows EC 50 value of 5.7 μM in L. donovani intramacrophage assay, where the amastigotes are cultured in differentiated THP-1 cells. GSK3494245 demonstrates good selectivity over mammalian cell growth inhibition (THP-1 cells; EC 50 > 50 μM). GSK3494245 (DDD01305143) shows pEC 50 s of 6.5 and 5.8 against axenic amastigote and ld InMac, respectively. Ld InMac is the intramacrophage assay carried out in THP-1 cells with L. donovani amastigote. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
GSK3494245 (25 mg/kg; orally twice a day for 10 consecutive days) elicits a >95% reduction of parasite load in Infected mice ( L. donovani , LV9) . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
Specifications
Specifiche e purezza
≥98%
Meccanismi biochimici e fisiologici
GSK3494245 (DDD01305143) is a potent, orally active, and selective inhibitor of the chymotrypsin-like activity of the parasite proteasome binding in a site sandwiched between the β4 and β5 subunits ( IC 50 =0.16 μM for WT L. donovani proteasomes). GSK3494
Condizioni di conservazione di stoccaggio
Store at -20°C
Spedito in
Ice chest + Ice pads
Questo prodotto richiede spedizione a catena fredda. I servizi di terra e altri servizi economici non sono disponibili.
Certificati (CoA, COO, BSE/TSE e tabella di analisi)
C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:
Proprietà chimiche e fisiche
Solubilità
DMSO : 100 mg/mL (243.64 mM; Need ultrasonic)
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Recensioni
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What is the purity of this product?
This product is supplied at ≥98% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.
How is this product shipped?
This product ships in an insulated container with ice pads. Unpack on arrival and transfer it to the storage condition stated above.
What are the CAS number, molecular formula and molecular weight?
The CAS Number is 2080410-41-7, the molecular formula is C21H23FN6O2, and the molecular weight is 410.44 g/mol.
How should this product be stored?
Store at ?20 °C. Freezer storage is required to maintain the specified shelf life.
What documentation is provided?
Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.
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