315183-21-2|PAC-1|PAC-1|MFCD02051977-范德生物科技公司

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PAC-1

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names：
PAC-1
CAS号：
315183-21-2
MDL Number： MFCD02051977
MF(分子式)： C23H28N4O2 MW(分子量)： 392.494
EINECS: Reaxys Number:
Pubchem ID:135421197 Brand:BIOFOUNT

PAC-1(315183-21-2,procaspase activating compound-1)是一种 procaspase-3 激活剂，诱导癌细胞凋亡，EC₅₀ 为 2.08 μM。PAC-1已用于研究淋巴瘤，黑素瘤，实体瘤，乳腺癌和胸癌等的治疗研究中。

货品编码	规格	纯度	价格 (¥)	现价(¥)	特价(¥)	库存描述	数量	总计 (¥)
HCC340301-5mg	5mg	97%	¥ 731.50	¥ 731.50		4-7周	- +	¥ 0.00

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中文别名	PAC-1(315183-21-2);PAC1; PAC 1；PAC1; VO-100; VO100; VO 100; procaspase激活化合物1;
英文别名	PAC-1(315183-21-2);PAC1; PAC 1; PAC1; VO-100; VO100; VO 100; procaspase activating compound-1;
CAS号	315183-21-2
SMILES	C=CCc1cccc(c1O)/C=N\NC(=O)CN2CCN(CC2)Cc3ccccc3
Inchi	InChI=1S/C23H28N4O2/c1-2-7-20-10-6-11-21(23(20)29)16-24-25-22(28)18-27-14-12-26(13-15-27)17-19-8-4-3-5-9-19/h2-6,8-11,16,29H,1,7,12-15,17-18H2,(H,25,28)/b24-16-
InchiKey	YQNRVGJCPCNMKT-JLPGSUDCSA-N
分子式 Formula	C23H28N4O2
分子量 Molecular Weight	392.494
闪点 FP	Not available
熔点 Melting point	Not available
沸点 Boiling point	Not available
Polarizability极化度	46.2±0.5 10-24cm3
密度 Density	1.1±0.1 g/cm3
蒸汽压 Vapor Pressure	Not available
溶解度Solubility	生物体外In Vitro:DMSO溶解度50 mg/mL(127.39 mM;Need ultrasonic)H2O< 0.1 mg/mL(insoluble)
性状	白色固体
储藏条件 Storage conditions	Store at +4°C，storage at -4℃ (1-2weeks), longer storage period at -20℃ (1-2years)

PAC-1(315183-21-2,procaspase activating compound-1)实验注意事项：
1.实验前需戴好防护眼镜，穿戴防护服和口罩，佩戴手套，避免与皮肤接触。
2.实验过程中如遇到有毒或者刺激性物质及有害物质产生，必要时实验操作需要手套箱内完成以免对实验人员造成伤害
3.实验后产生的废弃物需分类存储，并交于专业生物废气物处理公司处理，以免造成环境污染Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.

Tags:PAC-1试剂,PAC-1杂质,PAC-1中间体,PAC-1密度,PAC-1溶解度,PAC-1合成,PAC-1旋光度,PAC-1闪点,PAC-1购买,

产品说明	PAC-1(315183-21-2,procaspase activating compound-1)可以作为药物杂质对照品以及生物医药类试剂。
Introduction	PAC-1(315183-21-2,procaspase activating compound-1)can be used as a reference substance for drug impurities and reagents，only for research.
Application1
Application2
Application3

PAC-1(315183-21-2,procaspase activating compound-1)药理学：

1、PAC-1被称为首个激活蛋白酶的化合物，可选择性诱导癌细胞中的细胞凋亡或细胞自杀。PAC-1在小鼠模型中显示出良好的效果，并且正在进一步评估其在人类中的使用。2010年，一项发表的研究表明PAC-1对研究犬是安全的，同年晚些时候发表的第二项研究报告说，在一项小型的I期临床试验中，PAC-1衍生物（称为S-PAC-1）具有良好的耐受性。淋巴瘤的宠物狗。即使在低剂量的S-PAC-1中，肿瘤也会在1/6只狗中消退，并且在3/6只狗中疾病得以稳定（没有额外的肿瘤生长）。

2、PAC-1是caspase 3激活剂。Caspase激活是癌症治疗中的关键策略。半胱天冬酶3是关键的执行者半胱天冬酶和凋亡的直接效应子。许多癌症的标志是规避of子手胱天蛋白酶激活和凋亡反应丧失的信号。半胱天冬酶3激活的EC ₅₀ = 0.33μM，半胱天冬酶7 = 4.5μM。凋亡诱导的IC ₅₀ = 0.92μM。癌细胞系和组织中caspase 3的水平升高使PAC-1选择性地诱导组织中的细胞凋亡。

3、脯氨酸蛋白酶激活化合物1（PAC-1）是邻羟基N-酰基肼化合物。对多种癌细胞具有细胞毒性，例如淋巴瘤，白血病，乳腺癌和成胶质细胞瘤。高剂量的PAC-1可以促进神经兴奋。PAC-1有助于原酶蛋白酶的体外自激活，PAC-1可作为其他蛋白酶激活化合物的原型。 procaspase-3的PAC-1依赖性激活与锌的螯合有关。

警示图
危险性	warning
危险性警示	Not available
安全声明	H303+H313+H333
安全防护	P264+P280+P305+P351+P338+P337+P313
备注	实验过程中防止吸入、食入，做好安全防护

PAC-1(315183-21-2,procaspase activating compound-1)危害标识：

象形图


信号	Warning
GHS危险说明	Aggregated GHS information provided by 38 companies from 1 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.
	H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]
	H315 (100%): Causes skin irritation [Warning Skin corrosion/irritation]
	H319 (100%): Causes serious eye irritation [Warning Serious eye damage/eye irritation]
	H335 (100%): May cause respiratory irritation [Warning Specific target organ toxicity, single exposure; Respiratory tract irritation]
	H400 (100%): Very toxic to aquatic life [Warning Hazardous to the aquatic environment, acute hazard]
	Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown.
防范说明代码	P261, P264, P270, P271, P273, P280, P301+P312, P302+P352, P304+P340, P305+P351+P338, P312, P321, P330, P332+P313, P337+P313, P362, P391, P403+P233, P405, and P501
防范说明代码	(The corresponding statement to each P-code can be found at the GHS Classification page.)

Wang F, et al. A novel small-molecule activator of procaspase-3 induces apoptosis in cancer cells and reduces tumor growth in human breast, liver and gallbladder cancer xenografts. Mol Oncol. 2014 Dec

Seervi M, et al. ERO1α-dependent endoplasmic reticulum-mitochondrial calcium flux contributes to ER stress and mitochondrial permeabilization by procaspase-activating compound-1 (PAC-1). Cell Death Di

Putt KS, et al. Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy. Nat Chem Biol. 2006 Oct;2(10):543-50.

Parallel signaling pathways of pituitary adenylate cyclase activating polypeptide (PACAP) regulate several intrinsic ion channels PMID 31162688; Annals of the New York Academy of Sciences 2019 11; 145

Protamine stimulates platelet aggregation in vitro with activation of the fibrinogen receptor and alpha-granule release, but impairs secondary activation via ADP and thrombin receptors PMID 31992110;

PAC-1(315183-21-2,procaspase activating compound-1)参考文献：

1.The Effect of Regular Intake of Dry-Cured Ham Rich in Bioactive Peptides on Inflammation, Platelet and Monocyte Activation Markers in Humans.
Martínez-Sánchez SM;Minguela A;Prieto-Merino D;Zafrilla-Rentero MP;Abellán-Alemán J;Montoro-García S Nutrients. 2017 Mar 23;9(4). pii: E321. doi: 10.3390/nu9040321.

Background and aims;: Dietary studies have shown that active biopeptides provide protective health benefits, although the mediating pathways are somewhat uncertain. To throw light on this situation, we studied the effects of consuming Spanish dry-cured ham on platelet function, monocyte activation markers and the inflammatory status of healthy humans with pre-hypertension. ;Methods;: Thirty-eight healthy volunteers with systolic blood pressure of >125 mmHg were enrolled in a two-arm crossover randomized controlled trial. Participants received 80 g/day dry-cured pork ham of >11 months proteolysis or 100 g/day cooked ham (control product) for 4 weeks followed by a 2-week washout before "crossing over" to the other treatment for 4 more weeks. Soluble markers and cytokines were analyzed by ELISA. Platelet function was assessed by measuring P-selectin expression and PAC-1 binding after ADP (adenosine diphosphate) stimulation using whole blood flow cytometry. Monocyte markers of the pathological status (adhesion, inflammatory and scavenging receptors) were also measured by flow cytometry in the three monocyte subsets after the interventional period. ;Results;: The mean differences between dry-cured ham and cooked ham followed by a time period adjustment for plasmatic P-selectin and interleukin 6 proteins slightly failed (;p =; 0.

2.Localization of the pituitary adenylate cyclase-activating polypeptide receptor and its mRNA in the rat adrenal medulla.
Shioda S;Shimoda Y;Hori T;Mizushima H;Ajiri T;Funahashi H;Ohtaki K;Ryushi T Neurosci Lett. 2000 Dec 8;295(3):81-4.

We examined the localization of the pituitary adenylate cyclase-activating peptide (PACAP) receptor (PAC1-R) and its mRNA with immunocytochemistry and in situ hybridization, respectively. PAC1-R immunoreactivity and its transcript were detected in both chromaffin cells and ganglion cells but not detected in the adrenal cortex. In addition, strong PAC1-R immunoreactivity was found beneath the plasma membrane of the immunoreactive medullary cells. Electron microscopic immunocytochemistry revealed that PAC1-R was predominantly expressed in adrenaline-containing cells. This report supports the notion that PACAP is an activator and modulator of catecholamine secretion as well as synthesis in the adrenal medulla.

3.Magnitude and time course of platelet inhibition with Aggrenox and Aspirin in patients after ischemic stroke: the AGgrenox versus Aspirin Therapy Evaluation (AGATE) trial.
Serebruany VL;Malinin AI;Sane DC;Jilma B;Takserman A;Atar D;Hennekens CH Eur J Pharmacol. 2004 Sep 24;499(3):315-24.

The European Stroke Prevention Study showed greater stroke prevention for Aggrenox than either for aspirin or dipyridamole alone. To test whether Aggrenox has superior antiplatelet properties to aspirin alone we conducted the AGgrenox versus Aspirin Therapy Evaluation (AGATE) trial. Forty patients with prior ischemic stroke not taking aspirin for at least 30 days were randomized to Aggrenox (2 pills/daily) or aspirin (81 mg plus matching placebo/daily) for 30 days. Platelet function was assessed at baseline, 24 h, and days 3, 7, 15, and 30 by aggregometry, flow cytometry and cartridge-based analyzers. Both Aggrenox and aspirin provided fast and sustained platelet inhibition. Aggrenox(R), however, especially after 15 days, showed significant prolongation of the closure time (P=0.04), diminished expression of platelet/endothelial cell adhesion molecule-1 (PECAM-1) (P=0.01), glycoprotein IIb (GPIIb) antigen (P=0.02), and GPIIb/IIIa activity (P=0.01) by PAC-1 C antibody, CD63 (P=0.03), as well as inhibition of Protease Activated Receptors (PAR-1) associated with intact (SPAN12, P=0.01) and cleaved (WEDE15, P=0.01) thrombin receptors as compared with aspirin. Surprisingly, GPIb expression increased, especially after aspirin.

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