L-368,899 hydrochloride

Name: L-368,899 hydrochloride
Brand: Tocris Bioscience
SKU: 2641
Rating: 5 (1 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 2641

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Citations (27)

COA / SDS

Potent, non-peptide oxytocin receptor antagonist

Key Product Details

Description:	Potent, non-peptide oxytocin receptor antagonist
Chemical Name:	(2S)-2-Amino-N-[(1S,2S,4R)-7,7-dimethyl-1-[[[4-(2-methylphenyl)-1-piperazinyl]sulfonyl]methyl]bicyclo[2.2.1]hept-2-yl]-4-(methylsulfonyl)butanamide dihydrochloride
Purity:	≥97% (HPLC)
Molecular Weight:	627.68

View Full Technical Details for L-368,899 hydrochloride

Technical Data
Citations / Reviews (1)

Biological Activity for L-368,899 hydrochloride

L-368,899 hydrochloride is a potent, non-peptide and orally active oxytocin receptor antagonist (IC₅₀ = 8.9 nM) that displays > 40-fold selectivity over vasopressin V_1a and V₂ receptors (IC₅₀ values are 370 and 570 nM respectively). Antagonizes oxytocin-induced uterine contractions in vitro and in vivo.

Compound Libraries for L-368,899 hydrochloride

L-368,899 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for L-368,899 hydrochloride

M. Wt	627.68
Formula	C₂₆H₄₂N₄O₅S₂.2HCl
Storage	Store at -20°C
Purity	≥97% (HPLC)
PubChem ID	90488775
InChi Key	WJPIJZWOCNBGTR-HILSUTFGSA-N
Smiles	CC(C=CC=C1)=C1N2CCN(S(C[C@@]34CC[C@@H](C4(C)C)C[C@@H]3NC([C@@H](N)CCS(C)(=O)=O)=O)(=O)=O)CC2.Cl.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for L-368,899 hydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	water	59.12	100
	DMSO	59.12	100

Preparing Stock Solutions for L-368,899 hydrochloride

The following data is based on the product molecular weight 627.68.

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.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.59 mL	7.97 mL	15.93 mL
5 mM	0.32 mL	1.59 mL	3.19 mL
10 mM	0.16 mL	0.80 mL	1.59 mL
50 mM	0.03 mL	0.16 mL	0.32 mL

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References for L-368,899 hydrochloride

References are publications that support the biological activity of the product.

Borthwick Oral oxyt. antagonists. J.Med.Chem. 2010 PMID: 20550119
Mann Attenuation of PGE_2α release in ewes infused with the oxyt. antagonist L-368,899. Domest.Anim.Endocrinol. 2003 PMID: 14550509
Quattropani Discovery and development of a new class of potent, selective, orally active oxyt. receptor antagonist. J.Med.Chem. 2005 PMID: 16302826
Williams 1-(((7,7-dimethyl-2(S)-(2(S)-amino-4-(methylsulfonyl)butyramido)bicyclo[2.2.1]-heptan-1(S)-yl)methyl)sulfonyl)-4-(2-methylphenyl)piperazine (L-368,899): an orally bioavailable, non-peptide oxyt. antagonist with potential util J.Med.Chem. 1994 PMID: 8126695