Laniquidar

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

MedKoo CAT#: 205879

CAS#: 197509-46-9

Description: Laniquidar is a third-generation P-gp inhibitor, which has been used in clinic trials for modulating multidrug resistance transporters. A study of docetaxel in combination with the new orally administered P-glycoprotein (P-gp) inhibitor R101933 showed that this combination was feasible. However, due to the low oral bioavailability of R101933 and high interpatient variability, no further attempts to increase the level of P-gp inhibition were made.


Chemical Structure

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Laniquidar
CAS# 197509-46-9

Theoretical Analysis

MedKoo Cat#: 205879
Name: Laniquidar
CAS#: 197509-46-9
Chemical Formula: C37H36N4O3
Exact Mass: 584.28
Molecular Weight: 584.707
Elemental Analysis: C, 76.00; H, 6.21; N, 9.58; O, 8.21

Price and Availability

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Synonym: Laniquidar; R101933; R 101933; R-101933.

IUPAC/Chemical Name: methyl 11-(1-(4-(quinolin-2-ylmethoxy)phenethyl)piperidin-4-ylidene)-6,11-dihydro-5H-benzo[d]imidazo[1,2-a]azepine-3-carboxylate

InChi Key: TULGGJGJQXESOO-UHFFFAOYSA-N

InChi Code: InChI=1S/C37H36N4O3/c1-43-37(42)34-24-38-36-35(32-8-4-2-6-27(32)19-23-41(34)36)29-17-21-40(22-18-29)20-16-26-10-14-31(15-11-26)44-25-30-13-12-28-7-3-5-9-33(28)39-30/h2-15,24H,16-23,25H2,1H3

SMILES Code: O=C(C1=CN=C2N1CCC3=CC=CC=C3/C2=C4CCN(CCC5=CC=C(OCC6=NC7=CC=CC=C7C=C6)C=C5)CC\4)OC

Appearance: yellow 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, not in water

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 584.71 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: Moerman L, Dumolyn C, Boon P, De Vos F. The influence of mass of [11C]-laniquidar and [11C]-N-desmethyl-loperamide on P-glycoprotein blockage at the blood-brain barrier. Nucl Med Biol. 2012 Jan;39(1):121-5. Epub 2011 Sep 29. PubMed PMID: 21958857.