MK-0869 free base · Synonyms: MK-0869 | MK-869 | L-754030
Aprepitant is a selective and high-affinity neurokinin 1 receptor antagonist.
For research use only. Not for human or veterinary use.
MK-0869 structure
CAS No.: 170729-80-3
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| 5 g | USD 90.00 | BP-02465-5g | In stock | Get quote |
| 10 g | USD 160.00 | BP-02465-10g | In stock | Get quote |
| 20 g | USD 250.00 | — | In stock | Get quote |
| 50 g | USD 512.00 | — | In stock | Get quote |
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Description
Aprepitant (MK-0869) is a selective and high-affinity neurokinin 1 receptor antagonist with a Kd of 86 pM.
Biological activity
In Vitro Aprepitant decreases the metabolic activity with an estimated IC50 value of 20 μM. Aprepitant induces cell-growth inhibition and G1 cell-cycle arrest. Aprepitant significantly induces apoptosis in Nalm-6 cells, and the apoptosis is mediated through caspase-3 activation. Aprepitant (20 μM) induces p53 accumulation and expression of pro-apoptotic p53 target genes[2]. Aprepitant (1, 5, 10 μM) inhibits HIV infection in MDM from both depressed and not depressed HIV negative individuals ex vivo in a dose-dependent manner. IC90 value of aprepitant is equivalent to 10 μM, and the IC50 value is about 5 μM. In Vivo Aprepitant prevents the increase of NK-1R expression induced by in vivo NHP infection with B. burgdorferi. Aprepitant treatment prevents B. burgdorferi-induced increases in CCL2 protein levels in the CSF of NHPs. Aprepitant treatment prevents B. burgdorferi-induced increases in CCL2 and CXCL13 mRNA expression in the dorsal root ganglia of NHPs, prevents B. burgdorferi-induced increases in CCL2, CXCL13, IL-17A, and IL-6 mRNA expression in the spinal cord of NHPs. Aprepitant treatment attenuates B. burgdorferi infection-induced reductions in astrocyte activity/numbers[1]. Aprepitant (10 mg/kg, i.p.) significantly attenuates the CPP expression and locomotor activation produced by AMPH and cocaine in mice. Aprepitant does not induce significant CPP or conditioned place aversion or locomotor activation or suppression[3]. Aprepitant (125 mg/day, p.o.) results in 1 log reduction in plasma levels of viral RNA as compared to non-treated controls.
Identifiers
- SMILES
-
C[C@@H](O[C@H]1OCCN(CC2=NC(=O)NN2)[C@H]1C1=CC=C(F)C=C1)C1=CC(=CC(=C1)C(F)(F)F)C(F)(F)F - InChIKey
-
ATALOFNDEOCMKK-OITMNORJSA-N
Specifications
- MW (average)
- 534.4267
- Formula
- C23H21F7N4O3
- CAS No.
- 170729-80-3
- Physical state
- Solid
- Color
- White to off-white
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Powder 4°C, protect from light; In solvent -20℃ 1 month;
Solubility
Soluble in DMSO