HP661

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

MedKoo CAT#: 123463

CAS#: N/A

Description: HP661 is a highly potent and orally available OXPHOS inhibitor that effectively blocked the activity of mitochondrial complex I. HP661 specifically compromised the mitochondrial oxygen consumption of high-OXPHOS lung cancer cells but not that of low-OXPHOS lung cancer cells or normal cells in the low nanomolar range. Notably, mitogen-activated protein kinase kinase (MEK) inhibitor (trametinib)-resistant lung cancer cells with high levels of OXPHOS also showed marked sensitivity to HP661, as indicated by decreased clonogenic growth and increased cell apoptosis upon treatment. In a mouse model of high-OXPHOS lung cancer, HP661 treatment not only significantly suppressed tumor growth but also augmented the therapeutic efficacy of trametinib by impairing tumor mitochondrial respiration.

Chemical Structure

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HP661
CAS# N/A
Instruction

Theoretical Analysis

MedKoo Cat#: 123463
Name: HP661
CAS#: N/A
Chemical Formula: C31H29F6N7O3
Exact Mass: 661.22
Molecular Weight: 661.610
Elemental Analysis: C, 56.28; H, 4.42; F, 17.23; N, 14.82; O, 7.25

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Synonym: HP661; HP-661; HP 661;

IUPAC/Chemical Name: 5-((5-methyl-4-(4-(4-(2,2,2-trifluoroethoxy)benzyl)piperazine-1-carbonyl)-1H-1,2,3-triazol-1-yl)methyl)-N-(4-(trifluoromethyl)phenyl)picolinamide

InChi Key: ZMBFFBOMUBIJGL-UHFFFAOYSA-N

InChi Code: InChI=1S/C31H29F6N7O3/c1-20-27(29(46)43-14-12-42(13-15-43)17-21-2-9-25(10-3-21)47-19-30(32,33)34)40-41-44(20)18-22-4-11-26(38-16-22)28(45)39-24-7-5-23(6-8-24)31(35,36)37/h2-11,16H,12-15,17-19H2,1H3,(H,39,45)

SMILES Code: O=C(C1=NC=C(CN2N=NC(C(N3CCN(CC4=CC=C(OCC(F)(F)F)C=C4)CC3)=O)=C2C)C=C1)NC5=CC=C(C(F)(F)F)C=C5

Appearance: To be determined

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: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

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 661.61 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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He P, Feng J, Xia X, Sun Y, He J, Guan T, Peng Y, Zhang X, Liu M, Pang X, Chen Y. Discovery of a Potent and Oral Available Complex I OXPHOS Inhibitor That Abrogates Tumor Growth and Circumvents MEKi Resistance. J Med Chem. 2023 May 2. doi: 10.1021/acs.jmedchem.2c01844. Epub ahead of print. PMID: 37130350.