TRPV1

Voacapsacin（CA-008，Conentric镇痛药）是一种正在研究用于长期疼痛的TRPV激动剂，其作用机制与TRPV1相同，但其局部递送被认为可以最大限度地减少大量神经元的激活，如辣椒素局部产品[1]。

当注射到手术部位时，辣椒素会迅速转化为亲脂性辣椒素，并可以穿过膜到达TRVP1通道上所需的氨基酸靶点[1]。

[1]. Olivia Higgins, et al. Analgesics of the Future: The Potential of Vocacapsaicin Injections for Knee Pain. 12 Articles in Volume 21, Issue #2.

A recently completed Phase 2 clinical trial of vocacapsaicin displayed significant pain reductions in patients undergoing TKA. The study was randomized, double-blinded, and placebo-controlled. Every TKA patient received standard of care treatment, which included spinal anesthesia, ketorolac, acetaminophen, and ropivacaine in the form of joint filtration, femoral nerve, and IPACK blocks. Two intervention arms included administration of vocacapsaicin 36 mg (n = 61) and vocacapsaicin 60 mg (n = 62), each given via infiltration to the surgical site. The control arm (n = 64) received the standard of care regimen as well as opioid rescue as needed. The primary outcome was pain reductions recorded based on the numerical rating scale (NRS). The NRS is an 11-point scale with “0” being no pain and “10” being the most intense pain imaginable. The number being selected is expressed verbally by a patient based on the pain they have experienced in the last 24 hours. Pain reductions at rest – expressed when vocacapsaicin 36 mg was delivered – are displayed in Table I. Pain reductions with ambulation – when vocacapsaicin 36 mg was delivered – are expressed in Table II. Opioid consumption was significantly reduced among the vocacapsaicin 36-mg arm following a period of 96 hours and 168 hours after administration. Concentric Analgesics noted consistently better results with vocacapsaicin 36 mg compared to vocacapsaicin 60 mg. In light of side effect profiles, parameters among the intervention arms and control arm appeared consistent. Neither local nor systemic safety concerns were identified in the Phase 2 trial.¹⁴ A manuscript has yet to be published so further explanations of data including exclusion and inclusion criteria, definitions of AUC, specific adverse events, and rates, are not available. Further information will be welcomed to adequately assess the utilization of this therapy.

C26H42CLN3O4

496.08

495.28638

C, 62.95; H, 8.53; Cl, 7.15; N, 8.47; O, 12.90

1931116-92-5

Vocacapsaicin;1931116-86-7

132169136

Typically exists as solid at room temperature

79.9Ų

WOJDHHAJADLOCK-RVDQCCQOSA-N

InChI=1S/C26H41N3O4.ClH/c1-20(2)11-7-5-6-8-13-25(30)28-18-21-14-15-23(24(17-21)32-4)33-26(31)29-16-10-9-12-22(29)19-27-3;/h7,11,14-15,17,20,22,27H,5-6,8-10,12-13,16,18-19H2,1-4H3,(H,28,30);1H/b11-7+;

(E)-2-methoxy-4-((8-methylnon-6-enamido)methyl)phenyl 2-((methylamino)methyl)piperidine-1-carboxylate hydrochloride

Vocacapsaicin hydrochloride; CA-008 HYDROCHLORIDE; 1931116-92-5; Vocacapsaicin (hydrochloride); Vocacapsaicin hydrochloride (USAN); Vocacapsaicin hydrochloride [USAN]; CHEMBL4594295; SCHEMBL19643643;

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

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注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

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口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

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注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。