L-771688

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L-771688 is a highly selective α1A-Adrenoceptor antagonist with a K_i of 0.43±0.02 nM.

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L-771688 Chemical Structure

CAS No. : 200050-59-5

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α adrenergic receptor β adrenergic receptor

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Description	L-771688 is a highly selective α1A-Adrenoceptor antagonist with a K_i of 0.43±0.02 nM.
IC₅₀ & Target	Ki: 0.43±0.02 nM (α1A-Adrenoceptor)^[1]
In Vitro	Specific [³H]L-771688 binding to cloned human α1A-Adrenoceptors is inhibited with high potency by subtype selective compounds, GG818 (K_i=0.026±0.002 nM) and L-771688 (K_i=0.052±0.008 nM) and subtype non-selective α1-adrenoceptor antagonists, prazosin (K_i=0.088±0.0.032 nM) and terazosin (K_i=1.8±0.65 nM). The relative amount of [³H]L-771688 (0.5 nM) binding in various rat tissue membranes is highest in submaxillary gland (9.5 pmol/g tissue), followed by brain (5.8 pmol/g tissue), vas deferens (4.3 pmol/g tissue), kidney (3.4 pmol/g tissue), heart (1.5 pmol/g tissue), urethra (1.1 pmol/g tissue) and prostate (0.88 pmol/g tissue). In contrast, low specific [³H]L-771688 binding is observed in rat urinary bladder (0.55 pmol/g tissue), liver (0.44 pmol/g tissue), aorta (0.11 pmol/g tissue) and spleen (0.11 pmol/g tissue)^[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. L-771688 Related Antibodies
Molecular Weight	557.59
Formula	C₂₈H₃₃F₂N₅O₅
CAS No.	200050-59-5
SMILES	O=C(C([C@H](C1=CC=C(F)C(F)=C1)N2C(NCCCN3CCC(C4=NC=CC=C4)CC3)=O)=C(COC)NC2=O)OC
Shipping	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation	Data Sheet (271 KB) Handling Instructions (2659 KB)
References	[1]. Chang RS, et al. In vitro studies on L-771,688 (SNAP 6383), a new potent and selective alpha1A-adrenoceptor antagonist. Eur J Pharmacol. 2000 Dec 15;409(3):301-12. [Content Brief]

Cell Assay
^[1]

[³H]L-771688 is prepared by a catalytic reduction of the precursor, L-797429, in the presence of tritium gas followed by preparative high pressure liquid chromatography. Receptor membranes are prepared for [³H]prazosin/[¹²⁵I]HEAT binding assays. To measure [³H]L-771688 binding, 980 μL of membranes (cloning human α1A or rat tissues) are added to triplicate tubes containing 10 μL of dimethyl sulfoxide (DMSO) (for total binding) or phentolamine (10 μM final concentration, for nonspecific binding) or tested compounds (at the desiring final concentrations) and 10 μL of [³H]L-771688 (0.3 to 0.6 nM final concentration for routine studies and 10 pM to 5 nM for saturation assays). [³H]L-771688 is diluted in DMSO/methanol/water (1:1:2) from stock solution to minimize its loss to the wall of test tubes. The binding reaction is conducted at 25°C for 1 h or various time intervals in the association rate studies^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

[1]. Chang RS, et al. In vitro studies on L-771,688 (SNAP 6383), a new potent and selective alpha1A-adrenoceptor antagonist. Eur J Pharmacol. 2000 Dec 15;409(3):301-12. [Content Brief]

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

L-771688200050-59-5L771688L 771688Adrenergic ReceptorBeta ReceptorInhibitorinhibitorinhibit

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L-771688

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