ACT-280778

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

MedKoo CAT#: 565043

CAS#: 1537197-53-7

Description: ACT-280778 is a potent L/T calcium channel blocker.

Chemical Structure

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ACT-280778
CAS# 1537197-53-7
Instruction

Theoretical Analysis

MedKoo Cat#: 565043
Name: ACT-280778
CAS#: 1537197-53-7
Chemical Formula: C41H51N3O12
Exact Mass: 0.00
Molecular Weight: 777.870
Elemental Analysis: C, 63.31; H, 6.61; N, 5.40; O, 24.68

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.

Request quote for custom synthesis

Synonym: ACT280778; ACT-280778; ACT 280778

IUPAC/Chemical Name: (1R,2R,4R)-2-(2-((3-(4,7-Dimethoxy-1H-benzo[d]imidazol-2-yl)propyl)(methyl)amino)ethyl)-5-phenylbicyclo[2.2.2]oct-5-en-2-yl Isobutyrate bis-maleate

InChi Key: XCOMDWDKJAXYDF-YCAFZAMQSA-N

InChi Code: InChI=1S/C33H43N3O4.2C4H4O4/c1-22(2)32(37)40-33(21-24-13-14-25(33)20-26(24)23-10-7-6-8-11-23)17-19-36(3)18-9-12-29-34-30-27(38-4)15-16-28(39-5)31(30)35-29;2*5-3(6)1-2-4(7)8/h6-8,10-11,15-16,20,22,24-25H,9,12-14,17-19,21H2,1-5H3,(H,34,35);2*1-2H,(H,5,6)(H,7,8)/b;2*2-1-/t24-,25-,33+;;/m1../s1

SMILES Code: O=C(O)/C=C\C(O)=O.O=C(O)/C=C\C(O)=O.CC(C)C(O[C@]1(CCN(CCCC2=NC3=C(OC)C=CC(OC)=C3N2)C)[C@@](CC4)([H])C=C(C5=CC=CC=C5)[C@@]4([H])C1)=O

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: >3 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 777.87 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: Abele S, Funel JA, Schmidt G, Moessner C, Schwaninger M, Marti R. Daring the Challenge and Thinking Big: The Value of Early Process R&D. Chimia (Aarau). 2016;70(7-8):502-11. doi: 10.2533/chimia.2016.502. Erratum in: Chimia (Aarau). 2016 Sep;70(9):634. PubMed PMID: 27561612.

2: Dingemanse J, Otasevic P, Shakeri-Nejad K, Klainman E, Putnikovic B, Kracker H, Mueller MS, Zimlichman R. Efficacy and safety of the dual L- and T-type calcium channel blocker, ACT-280778: a proof-of-concept study in patients with mild-to-moderate essential hypertension. J Hum Hypertens. 2015 Apr;29(4):229-35. doi: 10.1038/jhh.2014.79. Epub 2014 Sep 18. PubMed PMID: 25231512.

3: Mueller MS, Shakeri-Nejad K, Gutierrez MM, Krause A, Täubel J, Sanderson B, Dingemanse J. Tolerability and pharmacokinetics of ACT-280778, a novel nondihydropyridine dual L/T-type calcium channel blocker: early clinical studies in healthy male subjects using adaptive designs. J Cardiovasc Pharmacol. 2014 Feb;63(2):120-31. doi: 10.1097/FJC.0000000000000030. PubMed PMID: 24126567.