L755,507, CRISPR Editing Enhancer

L-755, 507 was previously characterized as a potent and selective β3 adrenergic receptor partial agonist with EC50 ~0.43 nM. It has > 1000 fold selectivity overβ1- and β2-adrenoceptors (EC50 ~ 580 nM and >10000 nM forβ1- and β2-adrenoceptors respectively). It stimulates lipolysis in rhesus adipocytes in vitro (EC50 = 3.9 nM). In a recent study, L-755, 507 was identified to enhance CRISPR-mediated homology-directed repair (HDR) efficiency in human induced pluripotent stem cells (iPSCs) and other cell types.

Product information

CAS Number: 159182-43-1

Molecular Weight: 584.73

Formula: C30H40N4O6S

Chemical Name: (S)-4-(3-hexylureido)-N-(4-(2-((2-hydroxy-3-(4-hydroxyphenoxy)propyl)amino)ethyl)phenyl)benzenesulfonamide

Smiles: CCCCCCNC(=O)NC1C=CC(=CC=1)S(=O)(=O)NC1C=CC(CCNC[C@H](O)COC2=CC=C(O)C=C2)=CC=1

InChiKey: NYYJKMXNVNFOFQ-MHZLTWQESA-N

InChi: InChI=1S/C30H40N4O6S/c1-2-3-4-5-19-32-30(37)33-24-10-16-29(17-11-24)41(38,39)34-25-8-6-23(7-9-25)18-20-31-21-27(36)22-40-28-14-12-26(35)13-15-28/h6-17,27,31,34-36H,2-5,18-22H2,1H3,(H2,32,33,37)/t27-/m0/s1

Technical Data

Appearance: Solid Power.

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

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

L-755, 507 was used at 1-5 µM final concentration in various in vitro assays.

In Vivo:

L-755, 507 stimulates metabolic rate by 30% after acute bolus intravenous administration of 0.1 mg/kg to rhesus monkeys.

References:

1. Fisher MH, et al. A selective human beta3 adrenergic receptor agonist increases metabolic rate in rhesus monkeys. (1998) J Clin Invest.101(11):2387-93.
2. Parmee ER, et al. Discovery of L-755,507: a subnanomolar human beta 3 adrenergic receptor agonist. (1998) Bioorg Med Chem Lett. 8(9):1107-12.
3. Yu C, et al. Small Molecules Enhance CRISPR Genome Editing in Pluripotent Stem Cells. (2015) Cell Stem Cell 16(2):142-7.

Products are for research use only. Not for human use.

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