2. Membrane Transporter/Ion Channel
  3. P-glycoprotein
  4. P-gp inhibitor 21

P-gp inhibitor 21 (Compound 56) is an inhibitor for P-glycoprotein (P-gp) transport, which reverses P-gp-mediated multidrug resistance (MDR) and exhibits antitumor efficacy in mice without significant cytotoxicity.

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P-gp inhibitor 21 Chemical Structure

P-gp inhibitor 21 Chemical Structure

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P-gp inhibitor 21 Related Antibodies

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Description

P-gp inhibitor 21 (Compound 56) is an inhibitor for P-glycoprotein (P-gp) transport, which reverses P-gp-mediated multidrug resistance (MDR) and exhibits antitumor efficacy in mice without significant cytotoxicity[1].

In Vitro

P-gp inhibitor 21 inhibits proliferations of cells KBV200 and NCI/ADR-RES (combined with VNR) with IC50s of 2.4 and 27.9 nM, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

P-gp inhibitor 21 Related Antibodies
In Vivo

P-gp inhibitor 21 (75 mg/kg, i.p.) inhibits tumor growth and restores the sensitivity of MDR tumors to the VNR in KBV200 xenograft BALB/c nude mice without significant toxicity[1].

Pharmacokinetic Analysis of P-gp inhibitor 21 in mice[1]

route Dose (mg/kg) T1/2 (h) Tmax (h) Cmax (ng/mL) AUClast (ng·h/mL) AUCinf_obs (ng·h/mL) CLobs (mL/min/kg) MRTinf_obs (h) Vss (mL/kg) F (%)
iv 1 - - 1260 1263 33.5 0.75 1528 -
po 30 0.25 34.4 32.3 43.4 - 3.11 - 0.09

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: KBV200 xenograft BALB/c nude mice[1]
Dosage: 75 mg/kg
Administration: i.p.
Result: Suppressed tumor growth without significant body weight loss.
Molecular Weight

458.63

Formula

C27H42N2O4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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P-gp inhibitor 21 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

P-gp inhibitor 21P-glycoproteinP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243KBV200BALB/c miceInhibitorinhibitorinhibit

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