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28

抑制剂 & 化合物

8

天然产物

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Cat. No. Product Name Target Signaling Pathways
T9921 Infliximab

TNF Apoptosis
Infliximab 是一种与 TNF-α特异性结合的嵌合单克隆 IgG1 抗体,可阻止 TNF-α与 TNFR1和 TNFR2 的相互作用,用于治疗克罗恩病和类风湿性关节炎。
T7502L PF 05089771

PF-05089771,PF05089771

Sodium Channel Membrane transporter/Ion channel
PF 05089771是具有口服有效的、选择性的 Nav1.7丙烯酰胺抑制剂。PF-05089771在疼痛和糖尿病神经性疾病的研究中具有价值。
T7502 PF 05089771 tosylate

Sodium Channel Membrane transporter/Ion channel
PF 05089771 tosylate 是口服有效的、选择性的Nav1.7丙烯酰胺抑制剂。PF 05089771 tosylate 具有用于疼痛和糖尿病神经性疾病的研究。
T10244 ACY-1083

HDAC Chromatin/Epigenetic; DNA Damage/DNA Repair
ACY-1083 是一种选择性和脑穿透性 HDAC6 抑制剂 (IC50:3 nM),可有效逆转化疗引起的周围神经病变。
T72282 Ebaresdax hydrochloride

Endogenous Metabolite Metabolism
Ebaresdax hydrochloride 具有镇痛活性,,可用于研究由I型或II型糖尿病引起的糖尿病性神经病变疼痛。
T5385 Radiprodil

RGH-896

NMDAR; iGluR Membrane transporter/Ion channel; Neuroscience
Radiprodil (RGH-896) 是一种具有口服活性的、NMDA 受体 NR2B 亚类的选择性拮抗剂。它有用于神经性疼痛和其它慢性疼痛的相关研究潜力。
T21389 Enprofylline

Enprofilina,3-propylxanthine,3-n-Propylxanthine,Enprofyllinum,恩丙茶碱

Others Others
Enprofylline (Enprofilina) 是具有选择性的 A2B 受体竞争性拮抗剂 (Ki:7 μM) ,也是磷酸二酯酶抑制剂。它可用于研究哮喘、慢性阻塞性肺疾病。
T1458 Epalrestat

ONO2235,依帕斯他,依帕司他

Reductase Endocrinology/Hormones; Metabolism
Epalrestat (ONO2235) 是醛糖还原酶抑制剂,在长期治疗中具有良好的耐受性。 它可以有效改善糖尿病神经病变的相关症状并延缓疾病的进展,特别是在微血管病变有限且血糖控制良好的患者中。
T1993 J-147

J147

Epigenetic Reader Domain; Dopamine Receptor; Monoamine Oxidase Chromatin/Epigenetic; GPCR/G Protein; Neuroscience
J-147 是一种高效的、具有口服活性的、可透过血脑屏障神经保护剂,可增强认知能力。它抑制单胺氧化酶 B 和多巴胺转运体,EC50分别为 1.88 μM 和 0.649 μM。它有研究阿尔茨海默氏症的潜力。
T8644 Elamipretide Triacetate

Elamipretide TriTFA

Others Others
Elamipretide Triacetate (Elamipretide TriTFA) 是一种芳香族阳离子四肽,可轻松穿透细胞膜并短暂定位于线粒体内膜,在此与心磷脂结合。它已用于研究 Leber 遗传性视神经病变治疗的试验。
T39024 PrNMI

Cannabinoid Receptor GPCR/G Protein
PrNMI是一种针对外周限制性大麻素1受体(CB1R)的高效、口服活性激动剂。它展现出显著的镇痛特性,有效抑制化疗引起的周围神经病痛症状及癌症引起的骨痛。
T0976 Propoxur

残杀威,Aprocarb,Propoxure,Baygon

AChR; Antifungal Microbiology/Virology; Neuroscience
Propoxur (Propoxure) 是一种氨基甲酸酯类杀虫剂,用于控制蟑螂、苍蝇、蚊子以及草坪和草坪昆虫。
T68929 Lidorestat monohydrate

Lidorestat monohydrate is an aldose reductase inhibitor potentially for the treatment of diabetic neuropathy and diabetic complications.
T35299 Zenarestat

CI1014,FR74366,FK-366,CI-1014,FR 74366,FR-74366

Zenarestat (CI-1014, FK-366, FR-74366) is an aldose reductase inhibitor being studied as a treatment for diabetic neuropathy and cataracts.
T70579 SX 3202

SX 3202 is an aldose reductase inhibitor being developed for the treatment of diabetic neuropathy.
T28516 ReN-1869

NNC-05-1869,NNC 05-1869,NNC-051869,ReN 1869

ReN-1869 is a histamine H1 receptor antagonist. ReN 1869 is active against inflammation and neurogenic pain. ReN-1869 produces potent and selective antinociceptive effects on dorsal horn neurons after inflammation and neuropathy.
T82475 Emfilermin

Emfilermin,一种重组人白血病抑制因子 (LIF),适用于研究化疗引发的周围神经病变。
T81525 Pegylated synthetic human c-peptide

Pegylated synthetic human c-peptide 保留与天然(即非聚乙二醇化)C 肽相当的生物活性,且延长了在血浆中的循环停留时间,适用于糖尿病性周围神经病变的研究。
T62965 TDP1 Inhibitor-2

TDP1 Inhibitor-2 是一种 TDP1 (酪氨酰 -DNA 磷酸二酯酶 1) 的有效抑制剂 (IC50: 99 nM)。TDP1 Inhibitor-2 对 SCAN1 (脊髓小脑共济失调综合征伴轴突神经病变) 具有抑制作用 (IC50: 3.5 μM)。
T79303 IACS-52825

IACS-52825是一种选择性DLK抑制剂,具有1.3 nM的Kd值,适用于研究化疗引起的周围神经病变。
T62670 Cemdomespib

Cemdomespib (KU-596) 是一种高效的二代 Hsp90 调节剂。Cemdomespib 能够诱导热休克反应,诱导 Hsp70 水平,具有神经保护作用。Cemdomespib 具有改善糖尿病周围神经病变模型感觉缺陷的疗效。
T28897 T-1095A

T 1095A,J1.265.331J

T-1095A is an active metabolite of T-1095, a potent and selective inhibitor of Na+-glucose cotransporters (SGLTs). Chronic administration of T-1095 (0.1% w w(-1) pellet chow, for 12 weeks) decreased blood glucose and haemoglobin A(1C) levels, and improved
T37554 Oleyl Anilide

AcylCoA:cholesterol acyltransferase (ACAT) is an intracellular cholesteryl ester synthase tied closely to the absorption of dietary cholesterol. Oleyl analide (OA) is a weak inhibitor of acylCoA:cholesterol acyltransferase (ACAT) with an IC50 of 26 μM. OA and the related glyceride dioleoyl phenylamino propane 1,2-diol have been linked to a syndrome of eosinophilia, excessive T-cell activation, and elevated interleukin-4 (IL-4), soluble IL-2R, and IL-5. The clinical consequences are an acute pulm...
T38214 1-Deoxysphingosine (m18:1(4E))

1-Deoxysphingosine (m18:1(4E))

1-Deoxysphingosine (m18:1(4E)) is an atypical sphingolipid that contains a double bond at the 4E native position and is formed when serine palmitoyltransferase condenses palmitoyl-CoA with alanine instead of serine during sphingolipid synthesis.1,2 Plasma levels of 1-deoxysphingosine (m18:1(4E)) are increased in patients with chronic idiopathic axonal neuropathy (CIAP) and diabetic distal symmetrical polyneuropathy (DSPN).3 |1. Steiner, R., Saied, E.M., Othman, A., et al. Elucidating the chemica...
T72623 Nampt activator-3

NAMPTactivator-3 是一种 NAT 衍生物,是一种 NAMPT 激活剂,EC50为 2.6 μM,KD 为 132 nM。NAMPTactivator-3 有效保护培养细胞免受 FK866 介导的毒性。NAMPTactivator-3 在化疗引起的周围神经病变 (CIPN) 小鼠模型中表现出强大的神经保护功效,没有任何明显的毒性。
T79717 mHTT-IN-2

Huntingtin Neuroscience
mHTT-IN-2(化合物27)作为mHTT的一种有效抑制剂,具有EC50值为0.066 μM,能够降低HTT RNA外显子[49-50]的规范剪接,从而调节HTT基因的剪接。在人类HD干细胞和BACHD小鼠模型上,mHTT-IN-2已显示出明显的体外及体内活性。此外,该化合物也被应用于研究与branaplam相关的周围神经病变。
T68743 AZD4877 HCl

AZD4877 is a synthetic kinesin spindle protein (KSP) inhibitor with potential antineoplastic activity. KSP inhibitor AZD4877 selectively inhibits microtubule motor protein KSP (also called kinesin-5 or Eg5), which may result in the inhibition of mitotic spindle assembly; activation of the spindle assembly checkpoint; induction of cell cycle arrest during the mitotic phase; and cell death in tumor cells that are actively dividing. Because KSP is not involved in postmitotic processes, such as neur...
T83688 R 715 TFA

[Ac-Lys-[D-βNal7,Ile8]des-Arg9]-BK,Ac-Lys-Arg-Pro-Pro-Gly-Phe-Ser-D2Nal-Ile-OH

R 715是一种布拉迪肾上腺素B1受体拮抗剂。它抑制在表达布拉迪肾上腺素B1受体的孤立人类脐带中由布拉迪肾上腺素引发的收缩(pA2 = 8.49)。R 715(200、400及600 µg/kg)通过尾部闪烁测试减少了由链脲佐菌素(STZ)诱导的糖尿病神经病变小鼠模型中尾部撤回的潜伏期。它还在以髓磷脂少突胶质细胞糖蛋白(MOG)(35-55)(MOG35-55)抗原肽诱导的实验性自体免疫性脑炎(EAE)小鼠模型中,通过每天1 mg/kg的剂量减少了后肢无力和瘫痪的发病率,改善对称步态,并减少脊髓炎症灶点数、神经元脱髓鞘以及病灶单核细胞侵袭。R 715(0.01 nmol/动物,脑室内)能在自发性高血压大鼠中降低平均动脉血压并增加心率。

化合物

Infliximab
Cat.No: T9921
Synonym:
Target: TNF
PF 05089771
Cat.No: T7502L
Synonym: PF-05089771,PF05089771
Target: Sodium Channel
PF 05089771 tosylate
Cat.No: T7502
Synonym:
Target: Sodium Channel
ACY-1083
Cat.No: T10244
Synonym:
Target: HDAC
Ebaresdax hydrochloride
Cat.No: T72282
Synonym:
Target: Endogenous Metabolite
Radiprodil
Cat.No: T5385
Synonym: RGH-896
Target: NMDAR, iGluR
Enprofylline
Cat.No: T21389
Synonym: Enprofilina,3-propylxanthine,3-n-Propylxanthine,Enprofyllinum,恩丙茶碱
Target: Others
Epalrestat
Cat.No: T1458
Synonym: ONO2235,依帕斯他,依帕司他
Target: Reductase
J-147
Cat.No: T1993
Synonym: J147
Target: Epigenetic Reader Domain, Dopamine Receptor, Monoamine Oxidase
Elamipretide Triacetate
Cat.No: T8644
Synonym: Elamipretide TriTFA
Target: Others
PrNMI
Cat.No: T39024
Synonym:
Target: Cannabinoid Receptor
Propoxur
Cat.No: T0976
Synonym: 残杀威,Aprocarb,Propoxure,Baygon
Target: AChR, Antifungal
Lidorestat monohydrate
Cat.No: T68929
Synonym:
Target:
Zenarestat
Cat.No: T35299
Synonym: CI1014,FR74366,FK-366,CI-1014,FR 74366,FR-74366
Target:
SX 3202
Cat.No: T70579
Synonym:
Target:
ReN-1869
Cat.No: T28516
Synonym: NNC-05-1869,NNC 05-1869,NNC-051869,ReN 1869
Target:
Emfilermin
Cat.No: T82475
Synonym:
Target:
Pegylated synthetic human c-peptide
Cat.No: T81525
Synonym:
Target:
TDP1 Inhibitor-2
Cat.No: T62965
Synonym:
Target:
IACS-52825
Cat.No: T79303
Synonym:
Target:
Cemdomespib
Cat.No: T62670
Synonym:
Target:
T-1095A
Cat.No: T28897
Synonym: T 1095A,J1.265.331J
Target:
Oleyl Anilide
Cat.No: T37554
Synonym:
Target:
1-Deoxysphingosine (m18:1(4E))
Cat.No: T38214
Synonym: 1-Deoxysphingosine (m18:1(4E))
Target:
Nampt activator-3
Cat.No: T72623
Synonym:
Target:
mHTT-IN-2
Cat.No: T79717
Synonym:
Target: Huntingtin
AZD4877 HCl
Cat.No: T68743
Synonym:
Target:
R 715 TFA
Cat.No: T83688
Synonym: [Ac-Lys-[D-βNal7,Ile8]des-Arg9]-BK,Ac-Lys-Arg-Pro-Pro-Gly-Phe-Ser-D2Nal-Ile-OH
Target:
Cat. No. Product Name Target Signaling Pathways
T4S0537 Neoline

Bullatine B,雪上一枝蒿乙素

Others Others
Neoline (Bullatine B) 是一种乌头根(PA) 的活性成分,可改善奥沙利铂引起的小鼠周围神经病变。它可用作标记化合物,从而测定用于研究神经性疼痛的 PA 产品的质量。
TN1308 6-Hydroxyflavanone

Others; Lipoxygenase; COX; GABA Receptor Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience; Others
6-Hydroxyflavanone 是从菖蒲叶中提取分离,通过靶向环氧合酶-2(COX-2),5-脂氧合酶(5-LOX)以及阿片类药物和 GABA-A 受体从而具有抗炎和抗神经性疼痛活性。6-Hydroxyflavanone 在链脲佐菌素诱导的糖尿病神经病变模型中具有抗伤害感受特性。
T5813 BYAKANGELICIN

Reductase Endocrinology/Hormones; Metabolism
Byakangelicin 是发现于当归根中的一种活性化合物,可作为调节剂,改善各种活性化合物 (Umb,Cur 和 Dox) 的脑积累,增强研究效果。它提高所有PXR 靶基因 (如MDR1) 的表达,并广泛的诱导药物-药物相互作用。它可抑制性激素的作用,可能会增加内源激素的分解代谢。
T5S0661 Koumine

Others Others
Koumine 是一种从钩吻中得到的生物碱,具有高效抗肿瘤活性,在肿瘤细胞中能够提高 Bax/Bcl-2 的蛋白比例和 caspase-3 的表达。在类风湿性关节炎动物模型中,它能够预防关节炎的发展。它具有抗焦虑、抗应激、抗银屑病作用,也可用于缓解疼痛的研究。
T16165 Myriocin

ISP-I,Thermozymocidin

HCV Protease; Antifungal Microbiology/Virology; Proteases/Proteasome
Myriocin (Thermozymocidin) 是一种从 Myriococcum albomyces 中得到的代谢产物,是一种丝氨酸-棕榈酰转移酶 (SPT) 抑制剂,具有潜在的抗肿瘤抗癌和抗寄生虫活性,通过 PI3K/Akt/mTOR 通路调节巨噬细胞极化和功能来抑制肿瘤生长。Myriocin 抑制 HCV 感染,可用于研究神经病变和真菌感染。
T2563 Acetyl-L-carnitine hydrochloride

Acetyl L-carnitine hydrochloride,O-Acetylcarnitine,乙酰-L-肉(毒)碱盐酸盐,O-acetyl-L-carnitine,O-Acetyl-L-carnitine hydrochloride

Others; Endogenous Metabolite Metabolism; Others
Acetyl-L-carnitine hydrochloride (Acetyl L-carnitine hydrochloride) 是一种由内源性左旋肉碱的乙酰化形式的盐酸盐组成的营养补充剂,具有潜在的神经保护、认知增强、抗抑郁和免疫调节活性。还可缓解化疗、糖尿病或其他疾病引起的周围神经病变。此外,乙酰左旋肉碱可能通过增加T淋巴细胞成熟来调节免疫反应,并可能下调促炎细胞因子对病毒(如SARS-CoV-2)的反应。它还可能破坏ACE2信号通路并抑制活性氧(ROS)的产生。
T3S0209 Vincristine

ERK; p38 MAPK; NF-κB; Akt; JNK; mTOR Cytoskeletal Signaling; MAPK; NF-κB; PI3K/Akt/mTOR signaling
Vincristine 与微管蛋白结合并抑制微管的形成,从而抑制癌细胞的有丝分裂。 Vincristine 可用作微管去稳定剂,用于研究治疗血液系统癌症,如白血病和淋巴瘤以及儿童肉瘤的相关研究。
TN2299 Vindesine

Others Others
Vindesine is a microtubule inhibitor and widely used to treat malignancies. Vindesine neuropathy seems to be the cause of the patient's neurological symptoms.

天然产物

Neoline
Cat.No: T4S0537
Synonym: Bullatine B,雪上一枝蒿乙素
Target: Others
6-Hydroxyflavanone
Cat.No: TN1308
Synonym:
Target: Others, Lipoxygenase, COX, GABA Receptor
BYAKANGELICIN
Cat.No: T5813
Synonym:
Target: Reductase
Koumine
Cat.No: T5S0661
Synonym:
Target: Others
Myriocin
Cat.No: T16165
Synonym: ISP-I,Thermozymocidin
Target: HCV Protease, Antifungal
Acetyl-L-carnitine hydrochloride
Cat.No: T2563
Synonym: Acetyl L-carnitine hydrochloride,O-Acetylcarnitine,乙酰-L-肉(毒)碱盐酸盐,O-acetyl-L-carnitine,O-Acetyl-L-carnitine hydrochloride
Target: Others, Endogenous Metabolite
Vincristine
Cat.No: T3S0209
Synonym:
Target: ERK, p38 MAPK, NF-κB, Akt, JNK, mTOR
Vindesine
Cat.No: TN2299
Synonym:
Target: Others
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