1. GPCR/G Protein Neuronal Signaling
  2. Adrenergic Receptor
  3. ADRA1D receptor antagonist 1 free base

ADRA1D receptor antagonist 1 (free base) (compound (R)-9s) is an orally active, potent and selective human α1D-adrenoceptor (α1D-AR) antagonist (Ki=1.6 nM). ADRA1D receptor antagonist 1 (free base) dose-dependently inhibits bladder contraction with an IC30 value of 15 nM. ADRA1D receptor antagonist 1 (free base) can be used in studies of overactive bladder disorders such as urinary urgency, frequency and incontinence.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (ADRA1D receptor antagonist 1) usually boasts enhanced water solubility and stability.

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ADRA1D receptor antagonist 1 free base Chemical Structure

ADRA1D receptor antagonist 1 free base Chemical Structure

CAS No. : 1191908-24-3

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Description

ADRA1D receptor antagonist 1 (free base) (compound (R)-9s) is an orally active, potent and selective human α1D-adrenoceptor (α1D-AR) antagonist (Ki=1.6 nM). ADRA1D receptor antagonist 1 (free base) dose-dependently inhibits bladder contraction with an IC30 value of 15 nM. ADRA1D receptor antagonist 1 (free base) can be used in studies of overactive bladder disorders such as urinary urgency, frequency and incontinence.

In Vivo

ADRA1D receptor antagonist 1 (free base) (10 µg/kg; p.o.; single) inhibits cyclophosphamide-induced urinary frequency in rats[1].
ADRA1D receptor antagonist 1 (free base) (4.4 µg/kg; i.v.; single) inhibits bladder contraction with an IC 30 value of 15 nM in rats[1].

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

Animal Model: Rats with cyclophosphamide-induced cystitis[1].
Dosage: 10 µg/kg
Administration: Oral administration; single
Result: Increased voiding intervals.
Animal Model: Rats with BOO (bladder outlet obstruction)[1].
Dosage: 4.4 µg/kg
Administration: Intravenous injection; single
Result: Dose-dependently decreased the non-voiding bladder contractions during urinary storage phase.
Molecular Weight

300.74

Formula

C15H13ClN4O

CAS No.
SMILES

O=C(C1=CC(Cl)=CN([C@@H](C2=CC=CC(C#N)=C2)C)C1=N)N

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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ADRA1D receptor antagonist 1 free base Related Classifications

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This equation is commonly abbreviated as: C1V1 = C2V2

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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.

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ADRA1D receptor antagonist 1 free base
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HY-148252
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