PGP-4008
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 406963

CAS#: 365565-02-2

Description: PGP-4008 is a selective inhibitor of P-glycoprotein (P-gp) that does not affect the activity of multidrug resistance-related protein 1 (MRP1). PGP-4008, in combination with doxorubicin showed inhibition of tumor growth.

Chemical Structure

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PGP-4008
CAS# 365565-02-2
Instruction

Theoretical Analysis

MedKoo Cat#: 406963
Name: PGP-4008
CAS#: 365565-02-2
Chemical Formula: C26H23N3O
Exact Mass: 393.18
Molecular Weight: 393.490
Elemental Analysis: C, 79.36; H, 5.89; N, 10.68; O, 4.07

Price and Availability

Size Price Availability Quantity
1mg USD 250 2 Weeks
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Synonym: PGP-4008; PGP 4008; PGP4008.

IUPAC/Chemical Name: N-[2,3-dihydro-1-(phenylmethyl)-1H-pyrrolo[2,3-b]quinolin-4-yl]-benzeneacetamide

InChi Key: HVIAKQBMYMKWII-UHFFFAOYSA-N

InChi Code: InChI=1S/C26H23N3O/c30-24(17-19-9-3-1-4-10-19)28-25-21-13-7-8-14-23(21)27-26-22(25)15-16-29(26)18-20-11-5-2-6-12-20/h1-14H,15-18H2,(H,27,28,30)

SMILES Code: O=C(NC1=C2C(N(CC3=CC=CC=C3)CC2)=NC4=CC=CC=C14)CC5=CC=CC=C5

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: 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 Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 393.49 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Huang L, Wang J, Chen WC, Li HY, Liu JS, Tao Jiang, Yang WD. P-glycoprotein expression in Perna viridis after exposure to Prorocentrum lima, a dinoflagellate producing DSP toxins. Fish Shellfish Immunol. 2014 Aug;39(2):254-62. doi: 10.1016/j.fsi.2014.04.020. PubMed PMID: 24811006.

2: Yoshino Y, Yuan B, Kaise T, Takeichi M, Tanaka S, Hirano T, Kroetz DL, Toyoda H. Contribution of aquaporin 9 and multidrug resistance-associated protein 2 to differential sensitivity to arsenite between primary cultured chorion and amnion cells prepared from human fetal membranes. Toxicol Appl Pharmacol. 2011 Dec 1;257(2):198-208. doi: 10.1016/j.taap.2011.09.006. PubMed PMID: 21945491; PubMed Central PMCID: PMC3470788.

3: Miettinen S, Grènman S, Ylikomi T. Inhibition of P-glycoprotein-mediated docetaxel efflux sensitizes ovarian cancer cells to concomitant docetaxel and SN-38 exposure. Anticancer Drugs. 2009 Apr;20(4):267-76. doi: 10.1097/CAD.0b013e328329977f. PubMed PMID: 19262372.

4: Karla PK, Earla R, Boddu SH, Johnston TP, Pal D, Mitra A. Molecular expression and functional evidence of a drug efflux pump (BCRP) in human corneal epithelial cells. Curr Eye Res. 2009 Jan;34(1):1-9. doi: 10.1080/02713680802518251. PubMed PMID: 19172464; PubMed Central PMCID: PMC4406241.

5: Anglicheau D, Pallet N, Rabant M, Marquet P, Cassinat B, Méria P, Beaune P, Legendre C, Thervet E. Role of P-glycoprotein in cyclosporine cytotoxicity in the cyclosporine-sirolimus interaction. Kidney Int. 2006 Sep;70(6):1019-25. PubMed PMID: 16837925.

6: Maines LW, Antonetti DA, Wolpert EB, Smith CD. Evaluation of the role of P-glycoprotein in the uptake of paroxetine, clozapine, phenytoin and carbamazapine by bovine retinal endothelial cells. Neuropharmacology. 2005 Oct;49(5):610-7. PubMed PMID: 15961125.

7: Lee BD, Li Z, French KJ, Zhuang Y, Xia Z, Smith CD. Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. J Med Chem. 2004 Mar 11;47(6):1413-22. PubMed PMID: 14998330.

8: Lee BD, French KJ, Zhuang Y, Smith CD. Development of a syngeneic in vivo tumor model and its use in evaluating a novel P-glycoprotein modulator, PGP-4008. Oncol Res. 2003;14(1):49-60. PubMed PMID: 14552591.