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29

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T83729	Tat-CIRP TFA Tat-Cold-inducible RNA Binding Protein
	Tat-CIRP是一种肽类抑制剂，用于抑制髓样分化2蛋白(MD-2，亦称淋巴细胞抗原96 [LY96])与寒冷诱导的RNA结合蛋白(CIRP)之间的蛋白-蛋白相互作用。它通过与MD-2结合，干扰MD-2与CIRP之间的相互作用，这一作用在共免疫沉淀实验中得到证实。在体内实验中，Tat-CIRP (10及20 mg/kg) 能够减少由中脑动脉闭塞(MCAO)引发的小鼠脑梗死体积。同样，在通过血栓引发脑梗死的恒河猴模型中，Tat-CIRP同样能减少脑梗死体积，并缩短患中风一侧手臂抓取并放下食物的时间。
T16483	PF-05105679	TRP/TRPV Channel	Membrane transporter/Ion channel
	PF-05105679 是一种特异性 TRPM8 拮抗剂 (IC50 = 103 nM)。 PF-05105679 可用于冷相关疼痛的研究。
T21419	Diphenhydramine 苯海拉明,Debendrin,PM 255,PM255,Dabylen,Syntedril,PM-255	Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Diphenhydramine (Syntedril) 是第一代具有抗胆碱能作用的H1 受体拮抗剂，它能透过血脑屏障。
T3267	Potassium guaiacolsulfonate hemihydrate 愈创木酚磺酸钾水合物,Potassium guaiacolsulfonate,Potassium 4-guaiacolsulfonate hemihydrate,愈创木酚磺酸钾	Antibacterial; Antibiotic	Microbiology/Virology
	Potassium guaiacolsulfonate hemihydrate (Potassium guaiacolsulfonate) 是一种芳香族磺酸，在医药中用作祛痰剂，可治疗急性呼吸道感染。它可松弛粘液，与其他药物合用，可治疗普通感冒、感染或过敏引起的咳嗽。
T0205	Brompheniramine maleate Dimotane,马来酸溴苯那敏,Rolabromophen,Brompheniramine hydrogen maleate,Dimetane	5-HT Receptor; Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Brompheniramine maleate (Dimotane) 是一种可口服的丙胺类抗组胺剂，具有抗胆碱能和抗抑郁作用，可用于过敏性鼻炎和缓解疼痛的研究。它是一种选择性组胺 H1 受体拮抗剂，Kd 为 6.06 nM。
T71759	Coldephnine
	Coldephnine is a aconitine-type norditerpenoid alkaloid used as a nicotinic acetylcholine (ACh) receptor antagonist.
T34154	Propoxate R 7464,R7464,R-7464	Others	Others
	Propoxate（R7464）是一种强效麻醉剂，可用于麻醉冷血脊椎动物。
T0464	Carbetapentane citrate 托可拉斯,Pentoxyverine citrate,咳必清	AChR	Neuroscience
	Carbetapentane citrate (Pentoxyverine citrate) 能够选择性抑制咳嗽中枢，具有轻度的阿托品样作用和局麻作用。
T76702	Sutimlimab	Complement System	Immunology/Inflammation
	Sutimlimab 是一种新型靶向补体蛋白 C1 的单克隆抗体。Sutimlimab 常当作 C1 抑制剂使用，用于治疗冷凝集素病相关溶血。
T4563	Thonzylamine neohetramine,松齐拉敏	Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Thonzylamine (neohetramine) 是可口服的H1组胺受体拮抗剂，具有抗组胺和抗过敏特性，可用于鼻充血、过敏性结膜炎和其他过敏性疾病的研究。
T1232	Mepyramine maleate 马来酸吡纳明,Pyrilamine maleate,吡拉明马来酸盐	Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Mepyramine maleate (Pyrilamine maleate) 是一种组胺 H1 拮抗剂，对 H1、H2 和 H3 受体的 Kd 值分别为 0.8、5200 和大于 3000 nM，对 H1 受体的 pKd 值为 9.4。它是感冒药的常见成分，具有温和的催眠特性和局部麻醉作用，可用于胃肠外和局部过敏。
TP2068L	Cyclotraxin B acetate(1203586-72-4 free base)	Trk receptor	Tyrosine Kinase/Adaptors
	Cyclotraxin B acetate(1203586-72-4 free base) 是 TrkB 受体的拮抗剂；抑制 BDNF 诱导的 TrkB 活性 (IC50 = 0.30 nM)。变构改变 TrkB 受体构象但不改变 BDNF 结合。防止 BDNF 引起的小鼠冷异常性疼痛。还显示在小鼠中表现出推定的抗焦虑特性。
T33947	PF-06445974 PF-6445974,PF6445974,PF06445974,PF 6445974
	PF-06445974 has good selectivity for PDE4D, excellent brain permeability, and has a high level of specific binding in the "cold tracer" study.
T33978	Phenindamine Tartrate Pernovine,Thephorin,Nolahist,Phenindamine,Plegine
	Phenindamine Tartrate is an antihistamine and anticholinergic drug closely related to cyproheptadine. It is used to treat symptoms of the common cold and allergies, such as sneezing, itching, rashes, and hives.
T67212	Ligustrazine HCl
	Ligustrazine Hydrochloride, is a natural substance discovered in the plant Ligusticum chuanxiong Hort. It inhibits platelet aggregation, improves atherosclerosis situation, protects endothelium injury, and has antithrombotic effects.in vivo,ligustrazine hydrochloride at 10 and 20 mg/kg produced significant analgesic effects against mechanical stimuli,and ligustrazine hydrochloride at 80 mg/kg, also significantly alleviated cold hypersensitivity manifested by reduction in cold vocalization temper...
T33538	Mycobactin S
	Mycobactin S is made from metabolic products of the acid-resistant form of Mycobacterium phlei, a tuberculosis bacillus derived originally from the cold-blooded sea turtle. Importantly, it is not based on cell wall fragments or killed bacteria.
T27025	Cizolirtine citrate E-4018,E4018,E 4018
	Cizolirtine is a calcitonin gene-related peptide antagonist. Cizolirtine may be useful for alleviating some neuropathic somatosensory disorders, in particular cold allodynia, with a reduced risk of undesirable side effects. Cizolirtine inhibits the spinal
TP2068	Cyclotraxin B
	Antagonist of TrkB receptors; inhibits BDNF-induced TrkB activity (IC50 = 0.30 nM). Allosterically alters TrkB receptor conformation but does not alter BDNF binding. Prevents BDNF-induced cold allodynia in mice. Also shown to exhibit putative anxiolytic p
T69127	Moxisylyte
	Moxisylyte, also known as thymoxamine, is a drug used in urology for the treatment of erectile dysfunction. It is an α1-adrenergic antagonist. Moxisylyte is also used for the short-term treatment of primary Reynaud's syndrome, a condition where the fingers and toes become discoloured in response to cold or emotional distress. Moxisylyte helps by improving blood circulation to the extremities. It is also used locally in the eye to reverse the mydriasis caused by phenylephrine and other sympathomi...
T35921	N-Oleoyl Valine
	N-Oleoyl valine is an endogenous N-acyl amine that acts as an antagonist at the transient receptor potential vanilloid type 3 (TRPV3) receptor, which is involved in thermoregulation. N-Oleoyl valine is increased in mice following cold exposure for up to at least 16 days. Acute lung injury in mice increases the concentration of N-Oleoyl valine in lung tissue. N-acyl amines also promote mitochondrial uncoupling.
T80154	TAT-CIRP
	TAT-CIRP为小肽，指Tat融合的冷诱导RNA结合蛋白。作为骨髓分化蛋白2（MD2）的抑制剂，该化合物对小鼠缺血性及出血性中风显示出显著的神经保护效果。
T71286	Guaifenesin-d3
	Guaifenesin-d3 is intended for use as an internal standard for the quantification of guaifenesin by GC- or LC-MS. Guaifenesin is an expectorant. It inhibits production of mucin 5AC (MUC5AC), reduces mucus viscosity and elasticity, and increases the mucociliary transport rate of endogenous particles in primary human tracheobronchial epithelial cells in a concentration-dependent manner. Guaifenesin increases phenol red secretion, a marker of expectorant activity, in rats.3 Formulations containing ...
T37201	CAY10787
	CAY10787 is an oxysterol and a negative allosteric modulator of GABAAreceptors.1,2It reduces GABA-induced currents in HEK cells expressing α1β1γ2or α4β3γ2subunit-containing GABAAreceptors (IC50s = 1.5 and 1 μM, respectively).2CAY10787 (500 nM) reduces GABA-induced depolarization of peptidergic and non-peptidergic nociceptors, C-LTMRs, and cold thermosensors in isolated mouse dorsal root ganglion (DRG) neurons.In vivo, CAY10787 (2, 10, and 50 mg/kg) increases latency to nocifensive behaviors in t...
T38045	Cholesterol β-D-Glucoside
	Cholesterol β-D-glucoside is a derivative of cholesterol that contains β-D-glucose . It is formed from cholesterol and glucosylceramide by β-glucosidase 1. It activates heat shock transcription factor 1 (Hsf1) in response to heat shock, which increases the expression of heat shock protein 70 (Hsp70) in TIG-3 human fetal lung fibroblasts when used at a concentration of 10 μM. Cholesterol β-D-glucoside (100 mg/kg) prevents ulcer formation following cold-restraint stress and increases Hsf1 activity...
T71955	C3001a
	C3001a is a selective activator for TREK, against other two-pore domain K+(K2P) channels. C3001a binds to the cryptic binding site formed by P1 and TM4 in TREK-1. C3001a targets TREK channels in the peripheral nervous system to reduce the excitability of nociceptive neurons. In neuropathic pain, C3001a alleviated spontaneous pain and cold hyperalgesia. In a mouse model of acute pancreatitis, C3001a alleviated mechanical allodynia and inflammation. C3001a represents a lead compound which could a...
T38109	Galanin (2-11) amide (human, mouse, rat, porcine, bovine, ovine) (trifluoroacetate salt)
	Galanin (2-11) amide is a synthetic peptide fragment of the neuropeptide galanin and an agonist of the galanin-2 (GAL2) receptor (EC50= 9.32 nM in a fluorescence imaging plate reader assay).1It selectively binds to the GAL2receptor (IC50= 1.76 nM for the rat receptor) over the GAL1receptor (IC50= 879 nM for the human receptor) but does also bind to the GAL3receptor (Ki= 271 nM for the rat receptor).1,2Intracerebroventricular administration of galanin (2-11) amide (1 nmol/animal) decreases immobi...
T32091	Hofman's Violet
	Hoffman's violet is specific stains for animal chromosomes. Iodinated alcohol after staining can be substituted with various acids, both organic as well as inorganic, all of which act as trapping agent preventing leaching of the dye that binds with the ch
T81932	LIN28-IN-1
	LIN28-IN-1（compound 5）是针对RNA结合蛋白LIN28的抑制剂，可与LIN28的冷休克结构域（CSD）发生结合。该化合物能有效阻断LIN28与let-7miRNA的交互作用，具有显著的IC50值为5.4 μM，从而抑制LIN28在表观遗传学中的负向调控功能。此外，LIN28-IN-1在IC50为6.4 μM的条件下，显著抑制了过表达LIN28的JAR癌细胞的增殖。
T35457	(±)12(13)-DiHOME (±)12(13)-DiHOME,Isoleukotoxin diol
	(±)12(13)-DiHOME is the diol form of (±)12(13)-EpOME , a cytochrome P450-derived epoxide of linoleic acid also known as isoleukotoxin. [1] It is formed from 12(13)-EpOME by soluble epoxide hydrolase (sEH) in neutrophils. [2] 12(13)-DiHOME is toxic to Sf21 cells expressing sEH and to lacZ-expressing control cells, unlike isoleukotoxin, which is only toxic to cells containing sEH.[1] [2] Levels of 12(13)-DiHOME are increased in rat spinal cord following burn injury, and it enhances cold tolerance...

化合物

Cat.No: T83729

Synonym: Tat-Cold-inducible RNA Binding Protein

Cat.No: T16483

Target: TRP/TRPV Channel

Diphenhydramine

Cat.No: T21419

Synonym: 苯海拉明,Debendrin,PM 255,PM255,Dabylen,Syntedril,PM-255

Target: Histamine Receptor

Potassium guaiacolsulfonate hemihydrate

Cat.No: T3267

Synonym: 愈创木酚磺酸钾水合物,Potassium guaiacolsulfonate,Potassium 4-guaiacolsulfonate hemihydrate,愈创木酚磺酸钾

Target: Antibacterial, Antibiotic

Brompheniramine maleate

Cat.No: T0205

Synonym: Dimotane,马来酸溴苯那敏,Rolabromophen,Brompheniramine hydrogen maleate,Dimetane

Target: 5-HT Receptor, Histamine Receptor

Cat.No: T71759

Cat.No: T34154

Synonym: R 7464,R7464,R-7464

Target: Others

Carbetapentane citrate

Cat.No: T0464

Synonym: 托可拉斯,Pentoxyverine citrate,咳必清

Target: AChR

Cat.No: T76702

Target: Complement System

Cat.No: T4563

Synonym: neohetramine,松齐拉敏

Target: Histamine Receptor

Mepyramine maleate

Cat.No: T1232

Synonym: 马来酸吡纳明,Pyrilamine maleate,吡拉明马来酸盐

Target: Histamine Receptor

Cyclotraxin B acetate(1203586-72-4 free base)

Cat.No: TP2068L

Target: Trk receptor

Cat.No: T33947

Synonym: PF-6445974,PF6445974,PF06445974,PF 6445974

Phenindamine Tartrate

Cat.No: T33978

Synonym: Pernovine,Thephorin,Nolahist,Phenindamine,Plegine

Ligustrazine HCl

Cat.No: T67212

Cat.No: T33538

Cizolirtine citrate

Cat.No: T27025

Synonym: E-4018,E4018,E 4018

Cat.No: TP2068

Cat.No: T69127

N-Oleoyl Valine

Cat.No: T35921

Cat.No: T80154

Cat.No: T71286

Cat.No: T37201

Cholesterol β-D-Glucoside

Cat.No: T38045

Cat.No: T71955

Galanin (2-11) amide (human, mouse, rat, porcine, bovine, ovine) (trifluoroacetate salt)

Cat.No: T38109

Hofman's Violet

Cat.No: T32091

Cat.No: T81932

(±)12(13)-DiHOME

Cat.No: T35457

Synonym: (±)12(13)-DiHOME,Isoleukotoxin diol

Cat. No.	Product Name	Target	Signaling Pathways
T3370	Hederacoside C 常春藤苷C,Kalopanaxsaponin B,Hederasaponin C	Others; Antibacterial	Microbiology/Virology; Others
	Hederacoside C (Hederasaponin C) 是常春藤的叶子组分中的主要成分，具有祛痰、抗菌、支气管扩张等作用，可研究呼吸系统疾病。
T9790	Lactoferrin Lactoferrin (Bovine)	Endogenous Metabolite	Metabolism
	Lactoferrin 由哺乳动物分泌，具有广泛的生物学作用，包括提高应用良好的益生菌菌株的耐寒性。
T0330	Diphenhydramine hydrochloride 盐酸苯海拉明,Diphenhydramine HCl,DPH	Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Diphenhydramine hydrochloride (DPH) 是一种组胺 H1 拮抗剂，用作镇咳药和止吐药。它还用于治疗瘙痒和皮肤病、过敏反应、抗帕金森病、催眠药和普通感冒制剂的成分。
T37280	PE(18:1(9Z)/0:0)	Endogenous Metabolite	Metabolism
	PE(18:1(9Z)/0:0) 是一种天然存在的溶血磷脂，是缩醛磷脂溶血磷脂酰乙醇胺的类似物。 PE(18:1(9Z)/0:0) 以浓度依赖性方式诱导 PC12 大鼠神经元细胞中细胞内钙的瞬时增加。 PE(18:1(9Z)/0:0) 增加 IL-4 和 IL-2 的产生，但不增加 IFN-γ 的产生。在小鼠血清中，PE(18:1(9Z)/0:0)（1 μg/动物）诱导 T 辅助细胞 2 反应。在寒冷暴露三天后，小鼠肩胛间棕色脂肪组织中的 PE(18:1(9Z)/0:0) 水平增加。
TN4465	Luvangetin	COX; Prostaglandin Receptor; Antifection	GPCR/G Protein; Immunology/Inflammation; Microbiology/Virology; Neuroscience
	Luvangetin may have anti-inflammatory activity, it can inhibit NO and PGE2 production in LPS-stimulated BV2 cells. Luvangetin shows significant protection against pylorus-ligated and aspirin-induced gastric ulcers in rats and cold restraint stress-induced

天然产物

Cat.No: T3370

Synonym: 常春藤苷C,Kalopanaxsaponin B,Hederasaponin C

Target: Others, Antibacterial

Cat.No: T9790

Synonym: Lactoferrin (Bovine)

Target: Endogenous Metabolite

Diphenhydramine hydrochloride

Cat.No: T0330

Synonym: 盐酸苯海拉明,Diphenhydramine HCl,DPH

Target: Histamine Receptor

PE(18:1(9Z)/0:0)

Cat.No: T37280

Target: Endogenous Metabolite

Cat.No: TN4465

Target: COX, Prostaglandin Receptor, Antifection

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