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製品番号: HY-182537

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Org 9616 bromide

Org 9616 bromide is a non-depolarizing neuromuscular blocker with a structure similar to Pancuroniam. Org 9616 bromide induces rapid-onset, short-duration neuromuscular blockade.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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CAS 番号: 119302-18-0
分子式: C₃₆H₆₁BrN₂O₄
分子量:665.78

保管条件:

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

Org 9616 bromide 構造式

CAS 番号: 119302-18-0

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生物活性

製品説明

Org 9616 bromide is a non-depolarizing neuromuscular blocker with a structure similar to Pancuroniam. Org 9616 bromide induces rapid-onset, short-duration neuromuscular blockade^[1].

Parmacokinetics

Species	Dose	Route	T_1/2 (Distribution)	T_1/2β	V₁	V_dss	CL	MRT
Cat^[1]	1.2 mg/kg	i.v.	2.5 min	25.9 min	149 mL/kg	346 mL/kg	28.2 mL/min/kg	11.1 min

体内実験

Org 9616 (1.2 mg/kg; i.v.; bolus) bromide produces short-duration neuromuscular blockade in intact cats, with a duration of action of 14.6 minutes at a 1.2 mg/kg i.v. bolus dose, and is cleared via biotransformation and biliary excretion^[1].
Org 9616 (1.2 mg/kg; i.v.; bolus) bromide produces short-duration neuromuscular blockade in cats with ligated renal pedicles, with a duration of action of 15.4 minutes at a 1.2 mg/kg i.v. bolus dose, and renal pedicle ligation shortens its recovery index while prolonging elimination half-life and mean residence time^[1].

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

Animal Model:

either sex, 2-4 kg^[1]
Dosage:

1.2 mg/kg
Administration:

i.v.; bolus
Result:

Achieved onset time to maximum twitch depression of 0.7 minutes.
Reached duration of action (time to 25% twitch recovery) of 14.6 minutes.
Attained recovery index (25-75% twitch recovery) of 6.3 minutes.
Excreted 4.6% of the dose unchanged in urine, 20.4% unchanged in bile, and left 4.2% unchanged in the liver over 8 hours.
Excreted 1.4% of the dose as the 3-desacetyl metabolite in urine, 15.3% in bile, and left 9.8% in the liver over 8 hours.
Achieved total recovery of parent drug plus metabolite of 65% of the injected dose.\nAchieved onset time to maximum twitch depression of 0.5 minutes.
Reached duration of action (time to 25% twitch recovery) of 15.4 minutes.
Attained recovery index (25-75% twitch recovery) of 3.8 minutes, which was significantly shorter than in cats with intact renal pedicles (P < 0.05).
Showed prolonged mean elimination half-life and longer mean residence time compared to cats with intact renal pedicles.
Excreted 27.7% of the dose unchanged in bile, and left 3.6% unchanged in the liver over 8 hours.
Excreted 19.1% of the dose as the 3-desacetyl metabolite in bile, and left 14.5% in the liver over 8 hours.
Achieved total recovery of parent drug plus metabolite of 55% of the injected dose.

化学情報

CAS 番号 119302-18-0
分子量 665.78
分子式 C₃₆H₆₁BrN₂O₄
SMILES

C[C@@]12[C@](C[C@H]([N+]3(CCCCC3)C)[C@H]2OC(CCC)=O)([H])[C@@]4([H])[C@]([C@@]5([C@@](C[C@@H]([C@@H](N6CCCCC6)C5)OC(C)=O)([H])CC4)C)([H])CC1.[Br-]
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[1]. Khuenl-Brady K, et al. The neuromuscular blocking effects and pharmacokinetics of ORG 9426 and ORG 9616 in the cat. Anesthesiology. 1990;72(4):669-674. [Content Brief]

[2]. Kooijman H, et al. The conformation of the A-ring fragment of neuromuscular blocking agents structurally related to pancuronium. X-Ray structure determinations, molecular mechanics calculations and molecular dynamics simulations[J]. Journal of the Chemical Society, Perkin Transactions 2, 1996 (10): 2133-2140.

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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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