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Cat. No.: HY-184377

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Ipravacaine

Name: Ipravacaine
Brand: MedChemExpress
SKU: HY-184377
Availability: PreOrder

(Synonyms: IQB-9302)

Ipravacaine (IQB-9302) is a long-acting amide-based local anesthetic. Ipravacaine blocks open-state hKv1.5, with stereoselective, time-dependent and voltage-dependent inhibitory effects, and exerts stronger activity on the R (+) enantiomer. Ipravacaine blocks Kv2.1, Kv4.3 and HERG potassium channels. Ipravacaine induces negative chronotropic effects, increases mean arterial pressure, and exhibits vasodilatory effects at high concentrations.

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CAS No.: 166181-63-1
화학식: C₁₈H₂₆N₂O
분자량:286.41

보관:

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

Ipravacaine Chemical Structure

CAS No.: 166181-63-1

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Biological Activity
- 제품 설명
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
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Biological Activity

제품 설명

Ipravacaine (IQB-9302) is a long-acting amide-based local anesthetic. Ipravacaine blocks open-state hKv1.5, with stereoselective, time-dependent and voltage-dependent inhibitory effects, and exerts stronger activity on the R (+) enantiomer.^[1] Ipravacaine blocks Kv2.1, Kv4.3 and HERG potassium channels. Ipravacaine induces negative chronotropic effects, increases mean arterial pressure, and exhibits vasodilatory effects at high concentrations^[1]^[2].

In Vitro

Ipravacaine (10-500 μM; ~12 min) exerts stereoselective, time- and voltage-dependent open-channel block on hKv1.5 channels stably expressed in Ltk7 cells, with R (+) Ipravacaine (K_D=17.8 μM) being 3.2 times more potent than S (-) Ipravacaine (K_D=58.6 μM)^[1].
The molecularly simulated aromatic ring-overlapping conformers of R (+) and S (-) Ipravacaine have N-substituents with opposite orientations, which explains their stereoselective blocking effect on hKv1.5 channels^[1].

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

In Vivo

Ipravacaine (0.1-10 mg/kg; intravenous injection; infused over 30 seconds, followed by infusion of 100 μl heparinized sodium chloride solution within 15 seconds; administered every 20 minutes) induces dose-dependent decreases in heart rate and increases in mean arterial pressure in anesthetized Sprague-Dawley rats, with a maximum heart rate reduction of 114 bpm and a maximum mean arterial pressure elevation of 20.7 mmHg; the 10 mg/kg dose is lethal (all exposed rats survive for >1.5 minutes after administration), while the 3 mg/kg dose is well tolerated^[2].

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

Animal Model:

Sprague-Dawley (3-month-old, 250-350 g, sex-matched, anaesthetised with sodium pentobarbital)^[3]
Dosage:

0.1 mg/kg; 0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg
Administration:

i.v.; over 30 seconds, followed by 100 μl heparinised sodium chloride infusion over 15 seconds; every 20 minutes
Result:

Produced a maximum decrease in heart rate of 114 bpm.
Produced a maximum increase in mean arterial pressure of 20.7 mmHg.
Caused all exposed rats to die within 2 minutes at 10 mg/kg, with all surviving more than 1.5 minutes post-dose.
Was well-tolerated without mortality at 3 mg/kg.

Chemical Information

CAS No. 166181-63-1
분자량 286.41
화학식 C₁₈H₂₆N₂O
SMILES

O=C(C1N(CC2CC2)CCCC1)NC3=C(C)C=CC=C3C
Synonyms

IQB-9302
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Handling Instructions (2659 KB)

References

[1]. González T, et al. Stereoselective effects of the enantiomers of a new local anaesthetic, IQB-9302, on a human cardiac potassium channel (Kv1.5). British journal of pharmacology. 2001 Jan;132(2):385-92. [Content Brief]

[2]. Gallego-Sandin S, et al. The comparative hemodynamic effects of intravenous IQB-9302 and bupivacaine in anesthetized rats. Acta Anaesthesiol Scand. 2004 May;48(5):607-12. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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