PACAP 6-38
目录号 : GC10061
A PACAP receptor antagonist
Cas No.:143748-18-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | PC12 cells (5×104 cells per well) are deposited in a 96-well flat-bottom culture plate. Cells are incubated with PACAP(6-38) (0.1 and 1.0 μM) for 2 h before the addition of Dexamethasone (DEX, 1 μM). Cells are harvested at 24 h later of treatment. At regular intervals after the additional treatments, 100 μL of 0.2 mg/mL MTT is added per each well, and cells are incubated for 3 h at 37°C. After incubation, the MTT reagent is discarded, and 100 μL of DMSO is then added. The experiment is performed at room temperature for 20 min. The absorbance is then measured with SPECTRA max 340PC ELISA reader at the wavelength of 570 nm[2]. |
Animal experiment: | Mice[3]Two groups of mice are evaluated: WT mice receiving intravesical administration of vehicle (0.9% saline) and PACAP (6-38) (300 nM) (n=8) and NGF-OE mice receiving intravesical administration of vehicle (0.9% saline) and PACAP (6-38) (300 nM) (n=8). For intravesical administration of PACAP (6-38), mice are anesthetized with 2% isoflurane and PACAP (6-38) (<1.0 mL) is injected through the bladder catheter; the animals are maintained under anesthesia to prevent expulsion of PACAP (6-38) via a voiding reflex. In this procedure, PACAP (6-38) remains in the bladder for 30 min at which time, the drug is drained, the bladder washed with saline and animals recover from anesthesia for 20 min before experimentation[3]. |
References: [1]. Gourlet P, et al. Fragments of pituitary adenylate cyclase activating polypeptide discriminate between type I and II recombinant receptors. Eur J Pharmacol. 1995 Dec 4;287(1):7-11. | |
PACAP (6-38), human, ovine, rat is a potent PACAP receptor antagonist with IC50s of 30, 600, and 40 nM for PACAP type I receptor, PACAP type II receptor VIP1, and PACAP type II receptor VIP2, respectively.
An increase of dopamine (DA) content by HPLC analysis and/or cell proliferation identified by MTT assay by Dexamethasone (DEX) is also observed which can be inhibited by PACAP (6-38) at concentration sufficient to block PACAP type 1 (PAC1) receptor. Pretreatment with PAC1 receptor antagonist PACAP (6-38) at 0.1 or 1 μM for 2 h significantly blocks this increase of DA content by 1 μM DEX. The MTT assay shows that DEX increases cell proliferation. Moreover, this action is also inhibited by the pre-incubation of PACAP (6-38). PACAP (6-38) at 1μM shows no effect on DA content and cell proliferation for 24 h. However, PACAP (6-38) at 0.3 μM has been mentioned to reduce the spontaneous tyrosine hydroxylase (TH) accumulation in differentiated retinal cultured cells for 5 days[2].
Intravesical administration of the PAC1 receptor antagonist, PACAP (6-38) (300 nM), significantly (p≤0.01) increases intercontraction interval (2.0-fold) and void volume (2.5-fold) in NGF-OE mice. Intravesical instillation of PACAP (6-38) also decreases baseline bladder pressure in NGF-OE mice. Intravesical administration of PACAP (6-38) (300 nM) significantly (p≤0.01) reduces pelvic sensitivity in NGF-OE mice but is without effect in WT mice[3].
Reference：
[1]. Gourlet P, et al. Fragments of pituitary adenylate cyclase activating polypeptide discriminate between type I and II recombinant receptors. Eur J Pharmacol. 1995 Dec 4;287(1):7-11.
[2]. Yang TT, et al. Changes of dopamine content and cell proliferation by dexamethsone via pituitary adenylate cyclase-activating polypeptide in PC12 cell. Neurosci Lett. 2007 Oct 9;426(1):45-8.
[3]. Girard BM, et al. Intravesical PAC1 Receptor Antagonist, PACAP(6-38), Reduces Urinary Bladder Frequency and Pelvic Sensitivity in NGF-OE Mice. J Mol Neurosci. 2016 Jun;59(2):290-9.
| Cas No. | 143748-18-9 | SDF | |
| 分子式 | C182H300N56O45S | 分子量 | 4024.78 |
| 溶解度 | Soluble to 2 mg/ml in sterile water | 储存条件 | Desiccate at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.2485 mL | 1.2423 mL | 2.4846 mL |
| 5 mM | 0.0497 mL | 0.2485 mL | 0.4969 mL |
| 10 mM | 0.0248 mL | 0.1242 mL | 0.2485 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
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2.
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