Gsk-2250665a, an Itk inhibitor with pKi = 9.2, shows Itk selectivity against Aurora B kinase and Btk (pIC50 values 6.4 and 6.5, respectively) and a group of other kinases. Inhibit IFNγ production in PBMC.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Related Enzymes & Coenzymes Products|
|T7 RNA Polymerase（E. coli）
T7 RNA polymerase is a DNA-dependent RNA polymerase that specifically recognizes the T7 promoter sequence (5' -TaatacgactCactatagggaga-3 ') and has high specificity for the phage T7 promoter sequence. T7 RNA polymerase can catalyze NTP incorporation of single or double stranded DNA template downstream of T7 promoter to synthesize RNA complementary to the downstream DNA template of T7 promoter.
Ehp-101 (VCE-004.8) is an orally effective, specific PPARγ and CB2 receptor dual agonist. HP-101 inhibits prolyl - hydroxylase (PHDs) and activates the HIF pathway. HP-101 is a semi-synthetic, multi-target cannabinoid with potent anti-inflammatory activity.
Ralaniten triacetate (EPI-506), a prodrug for Ralaniten, is a pioneering, orally active androgen receptor (AR) N-terminal domain (NTD) inhibitor. Ralaniten triacetate is active against full-length and resistance-related AR species, including AR-v7.
Atabecestat (JNJ-54861911) is a potent brain-osmotic and has oral activity β-position amyloid precursor protein lyase 1 (BACE1 inhibitors that strongly reduce the expression of Aβ protein in cerebrospinal fluid. Atabecestat (JNJ-54861911) is tolerant and has sustained pharmacokinetic (PK) and pharmacodynamic (PD) profiles. Atabecestat (JNJ-54861911) has the potential to be used in the study of Alzheimer's disease.
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