Vapreotide acetate (BMY-41606 acetate; RC160 acetate) is a neurokinin-1 (NK1) receptor antagonist with IC50 value of 330 nM. Vapreotide inhibits SP-induced IL-8 and MCP-1 production in HEK293-NK1R and U373MG cell lines. Vapreotide also inhibits HIV-1 infection of human MDM in vitro, an effect that is reversible by SP pretreatment. Vapreotide inhibits serum-induced proliferation of CHO cells expressing SSTR2 and SSTR5 with EC50 of 53 and 150 pM, respectively.
| Molecular Weight | 1191.39 |
| Formula | C59H74N12O11S2 |
| CAS Number | 849479-74-9 |
| Solubility (25°C) | Water 11 mg/mL |
| Storage | -20°C, 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.
| Related Neurokinin Receptor Products |
|---|
| Spantide II
Spantide II, an undecapeptide substance P (SP) analog, is a potent neurokinin-1 receptor (NK-1R) antagonist. |
| Substance P (7-11)
Substance P (7-11) is a C-terminal fragment of Substance P which can cause an increase in the intracellular calcium concentration. |
| [Sar9, Met(O2)11]-Substance P TFA
[Sar9,Met(O2)11]-Substance P TFA is a tachykinin NK1 receptor selective agonist. |
| [bAla8]-Neurokinin A(4-10)
[bAla8]-Neurokinin A(4-10) is a neurokinin 2 (NK2) receptor agonist. |
| [Sar9, Met(O2)11]-Substance P
[Sar9,Met(O2)11]-Substance P is a tachykinin NK1 receptor selective agonist. |
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