Numidargistat (CB-1158) dihydrochloride is a potent and orally active inhibitor of arginase, with IC50s of 86 nM and 296 nM for recombinant human arginase 1 and recombinant human arginase 2, respectively. Immuno-oncology agent.
| Molecular Weight | 360.04 |
| CAS Number | 2095732-06-0 (free base) |
| Solubility (25°C) | DMSO 55 mg/mL Water 37.78 mg/mL |
| Storage | -20°C, dry, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| 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.
[1] Jonathan Wolf Mueller, et al. Steroid Sulfation in Adrenal Tumors
[2] Thomas Alec Lightning, et al. Steroid disulfates - Sulfation double trouble
[3] Zhengxiong Zhou, et al. [Production and application of 3-phosphoadenosine-5- phosphosulfate]
[4] Christine Kaufmann, et al. Sulfated plant peptide hormones
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