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Search Results for " experimental autoimmune encephalomyelitis "

29

抑制剂 & 化合物

2

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Cat. No.	Product Name	Target	Signaling Pathways
T24984	5J-4	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	5J-4 是一种有效的钙释放激活钙通道 (CRAC) 和钙池操纵性钙内流(SOCE) 阻滞剂。 5J-4 减少 IL-17 的产生并降低 RORα 和 RORγt 的表达。
T28169	NIBR-0213 NIBR 0213	LPL Receptor	GPCR/G Protein
	NIBR-0213 是S1P1选择性拮抗剂，有抗实验性自身免疫性脑脊髓炎的作用。在 GTPγ35S 试验中，它作用于人和大鼠S1P1的IC50分别为 2.0 nM 和 2.3 nM。
T14924	Cenerimod ACT-334441	S1P Receptor	GPCR/G Protein
	Cenerimod (ACT-334441) 是一种具有口服活性、选择性和高效性的磷酸鞘氨醇 1 受体（S1P1）激动剂（EC50：1 nM）。Cenerimod 对多种 S1P 的亚型具有抑制作用，可用于研究鼠类实验性自身免疫性脑脊髓炎 (EAE)和鼠类硬皮病。
T10385	ASP-4058	S1P Receptor; LPL Receptor	GPCR/G Protein
	ASP-4058 是一种鞘氨醇磷酸受体 1 和 5 (S1P1 and S1P5) 的二代激动剂，具有选择性、安全性和口服活性。ASP-4058能改善小鼠实验性自身免疫性脑脊髓炎。
T15795	Luzindole N-乙酰-2-苄基色胺,N-0774	Melatonin Receptor; MT Receptor	GPCR/G Protein; Neuroscience
	Luzindole (N-0774) 是一种选择性褪黑素受体拮抗剂，可抑制实验性自身免疫性脑脊髓炎，有抗抑郁样活性。它优先靶向 MT2 (Mel1b)，对于人 MT2 和 MT1 的 Ki 值分别为 10.2 和 158 nM。
T21509	CA 074	Cysteine Protease	Proteases/Proteasome
	CA 074 是一种高效的组织蛋白酶B (cathepsin B) 抑制剂， Ki 值为2 to 5 nM。CA 074 抑制灵长类动物缺血性海马神经元死亡，可减轻 SJL/J 小鼠诱导的实验性自身免疫性脑脊髓炎的视网膜病变和视神经炎。
T3701	MCC950 CP-456773	NOD	Immunology/Inflammation; NF-κB
	MCC950 (CP-456773) 是NLRP3的选择性抑制剂，能够作用于BMDMs(IC50:7.5 nM) 和 HMDMs(IC50:8.1 nM)。
T22398	Phenidone 菲尼酮,1-phenyl-3-pyrazolidinone	Lipoxygenase; COX	Immunology/Inflammation; Metabolism; Neuroscience
	Phenidone (1-phenyl-3-pyrazolidinone) 是可口服发环氧化酶和脂氧合酶双重抑制剂，可改善实验性自身免疫性脑脊髓炎大鼠的瘫痪，降低自发性高血压大鼠的血压，可用作照片显像剂。
T30529	BMS-520
	BMS-520 is a potent, selective S1P1 agonist that has shown impressive efficacy when administered orally in a rat model of arthritis and in a mouse model of experimental autoimmune encephalomyelitis (EAE) with multiple sclerosis.
T81734	Myelin Basic Protein (1-11)
	Myelin Basic Protein (1-11) 是髓鞘碱性蛋白 (MBP) 的一个致脑炎表位，并且常用于诱导实验性自身免疫性脑脊髓炎 (EAE)。
TP2080	ADWX 1
	Potent and selective KV1.3 channel blocker (IC50 values are 0.0019 and 0.65 nM for KV1.3 and KV1.1, respectively). Inhibits CD4+ CCR7- T cell activation. Ameliorates rat experimental autoimmune encephalomyelitis, in a model for multiple sclerosis.
T69066	Forphenicine
	Forphenicine is a bacterial metabolite that has been found in S. fulvoviridis and an inhibitor of alkaline phosphatase (IC50 = 0.036 µg/ml for the chicken intestine enzyme). It inhibits the growth of HL-60 leukemia cells when used at a concentration of 10 µM. Forphenicine (50 and 500 µg/animal) increases survival in a guinea pig model of experimental autoimmune encephalomyelitis (EAE).
T63206	SR12418
	SR12418 是一种特异性的 REV-ERB 合成配体，能够作用于 REV-ERBα (IC50: 68 nM) 和 REV-ERBβ (IC50: 119 nM)，可用于研究实验性自身免疫性脑脊髓炎 (EAE) 和结肠炎。
T39110	MOG (35-55), human
	MOG (35-55), human, a constituent of central nervous system myelin, is distinguishable from mMOG (35-55) due to a proline-to-serine substitution at position 42. It possesses immunogenic properties and is partially cross-reactive with mMOG35–55. However, MOG (35-55), human does not induce encephalitogenic effects, and only elicits minimal clinical signs of EAE (experimental autoimmune encephalomyelitis) in comparison to the rodent peptide.
T78031	MOG peptide (35-55)
	MOG peptide (35-55) 是一段特定的髓鞘少突胶质细胞糖蛋白 (MOG) 免疫原肽的35至55氨基酸序列。该肽段具有针对CD4+T细胞的特异性活性，并可用于诱导实验性自身免疫性脑脊髓炎 (EAE) 的动物模型。
T82020	J5 peptide Myelin basic protein (85-99) antagonist
	J5 peptide是MBP抑制剂，竞争性阻断MBP85-99与HLA-DR2的结合。该肽段能减轻PLP139-151/MBP85-99诱导的小鼠实验性自身免疫性脑脊髓炎(EAE)。J5 peptide主要用于研究炎症和免疫疾病。
T63141	ASP-4058 hydrochloride
	ASP-4058 hydrochloride 是一种选择性的、口服具有活力的的鞘氨醇磷酸受体 1 和 5 (S1P1and S1P5) 的二代激动剂。ASP-4058 hydrochloride 安全性良好，能够改善小鼠实验性自身免疫性脑脊髓炎。
T82621	D359-0396	NOD-like Receptor (NLR)	Immunology/Inflammation
	D359-0396 是一种口服活性的 NLRP3 炎性体抑制剂，能有效抑制巨噬细胞焦亡（pyroptosis）以及 IL-1β 的释放，并阻止 NLRP3 和 ASC 的寡聚化，抑制 GSDMD 的裂解。该化合物在动物模型中能减轻小鼠的 EAE 症状，并提高感染性休克后的小鼠存活率。
T72017	6(5H)-Phenanthridinone
	6(5H)-Phenanthridinone is an inhibitor of poly(ADP-ribose) polymerase 1 (PARP1) and PARP2. It decreases radiation-induced PARP activity and proliferation of RDM4 murine lymphoma cells. 6(5H)-Phenanthridinone reduces NF-κB-induced transcription of the genes encoding TNF-α, IL-2, and IFN-γ in rat lymphocytes. In vivo, 6(5H)-phenanthridinone reduces spinal cord expression of inducible nitric oxide synthase (iNOS), IL-1β, TNF-α, IL-2, and IFN-γ and reduces disease score in a rat model of experimenta...
T36015	PDMP (hydrochloride)
	PDMP is a ceramide analog first prepared in a search for inhibitors of glucosylceramide synthase. PDMP has two adjacent chiral centers (C1 and C2) allowing for the formation of four possible isomers. PDMP contains all four of these stereoisomers. PDMP inhibits glucosylceramide synthase by 90% when used at a concentration of 0.8 μM in MDCK cell homogenates, however, the ability to inhibit glucosylceramide synthase has been found to reside in the D-threo (1R,2R) enantiomer. The D-threo PDMP enanti...
T80682	γ-Fibrinogen 377-395 TFA
	γ-Fibrinogen377-395 TFA 是纤维蛋白原衍生抑制肽，具有纤维蛋白原表位特性。该化合物能在体外抑制小胶质细胞激活、阻断纤维蛋白与Mac-1相互作用，并在小鼠体内抑制实验性自身免疫性脑脊髓炎(EAE)。该肽适用于多发性硬化症(MS)及其他血脑屏障损伤和小胶质细胞激活相关的神经炎症疾病研究。
T80683	γ-Fibrinogen 377-395
	γ-Fibrinogen377-395是一种衍自纤维蛋白原的抑制性肽段，也被认为是纤维蛋白原的表位之一。它能在体外抑制小胶质细胞的激活并阻断纤维蛋白与Mac-1的交互作用；此外，在小鼠体内能够抑制实验性自身免疫性脑脊髓炎(EAE)的发展。因此，γ-Fibrinogen377-395对于多发性硬化症(MS)以及其他与血脑屏障损伤和小胶质细胞活化相关的神经炎症性疾病的研究具有潜在的应用价值。
T81772	MOG (92–106), mouse, rat
	MOG (92–106), mouse, rat 是一种来自小鼠/大鼠髓磷脂少突胶质细胞糖蛋白的生物活性肽，包含氨基酸片段92至106。在MOG (92–106) 诱导的实验性自身免疫性脑脊髓炎模型中，小鼠会对次级髓磷脂抗原呈现出广泛的B细胞反应性，尽管T细胞反应较弱。该肽段在SJL小鼠、DA大鼠以及恒河猴中均可诱导严重的脑炎。
T69600	Spermidine-d6
	Spermidine-d6 is intended for use as an internal standard for the quantification of spermidine by GC- or LC-MS. Spermidine is an endogenous polyamine. It is formed from putrescine by spermidine synthase. Spermidine (25 µM) inhibits the activity of the human inward-rectifying potassium channel Kir2.3 in a patch-clamp assay. It induces autophagy in HeLa cells when used at a concentration of 100 µM and increases the lifespan of D. melanogaster, yeast, and C. elegans. Spermidine (30 mM in the drinki...
T36296	BIO5192 hydrate
	BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 hydrate selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels[1][2]. The combination of BIO5192 hydrate (1 mg/kg; i.v.) and Plerixafor (5 mg/kg; s.c.) exert an additive effect on progenitor mobilization[1].BIO5192 hydrate (30 mg/kg; s.c; bid; during days...
T83690	[Leu144, Arg147]-PLP (139-151) TFA [Leu144, Arg147] Proteolipid Peptide (139-151),H-His-Ser-Leu-Gly-Lys-Leu-Leu-Gly-Arg-Pro-Asp-Lys-Phe-OH
	[Leu144,Arg147]-PLP (139-151)是髓鞘脂蛋白(PLP)的一种突变肽段，包含位于144和147位置的色氨酸到亮氨酸以及组氨酸到精氨酸的替换。使用[Leu144, Arg147]-PLP (139-151)（50 µg）乳化于完全弗氏佐剂(CFA)免疫后，能增加小鼠脾脏中的IL-4水平。它在体外抑制Th1细胞激活，但在体内不抑制，其中它诱导调节性T细胞的产生。用[Leu144, Arg147]-PLP (139-151)预免疫可以延迟由脑炎肽PLP (178-191)、髓磷脂少突细胞蛋白(MOG) (92-106)或髓鞘基础蛋白(MBP)在小鼠中诱导的实验性自身免疫性脑炎(EAE)的发病。
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。
T83910	S1PL-IN-31 Sphingosine-1-Phosphate Lyase Inhibitor 31,S1PL Inhibitor 31,S1P Lyase Inhibitor 31
	S1PL-IN-31是一种鞘氨醇-1-磷酸(S1P)裂解酶的抑制剂(IC50 = 210 nM)，同时也是Smoothened(Smo)受体的对抗剂(IC50 = 440 nM)。在体内，S1PL-IN-31 (每天2 mg/kg)能够防止实验性自身免疫性脑炎(EAE)模型大鼠中，由髓鞘少突胶质细胞糖蛋白(MOG)肽段MOG29-152诱发的颈部及胸部淋巴细胞渗透和神经肌肉虚弱。该化合物降低了大鼠的淋巴细胞总数及CD4+ T细胞、CD8+ T细胞和B细胞的水平。S1PL-IN-31 (每天3及10 mg/kg剂量)在雄性和雌性大鼠心脏和淋巴结中增加了S1P水平，并且在雌性大鼠中降低了心率。
T38106	JC-171
	JC-171 is a selective NLRP3 inflammasome inhibitor, with an IC50 of 8.45 μM for inhibiting LPS/ATP-induced interleukin-1β (IL-1β) release from J774A.1 macrophages[1]. JC-171 (0-100 μM) blocks NLRP3 inflammasome activation and IL-1β production in primary macrophages dose dependently[1]. ...

化合物

Cat.No: T24984

Target: Calcium Channel

Cat.No: T28169

Synonym: NIBR 0213

Target: LPL Receptor

Cat.No: T14924

Synonym: ACT-334441

Target: S1P Receptor

Cat.No: T10385

Target: S1P Receptor, LPL Receptor

Cat.No: T15795

Synonym: N-乙酰-2-苄基色胺,N-0774

Target: Melatonin Receptor, MT Receptor

Cat.No: T21509

Target: Cysteine Protease

Cat.No: T3701

Synonym: CP-456773

Target: NOD

Cat.No: T22398

Synonym: 菲尼酮,1-phenyl-3-pyrazolidinone

Target: Lipoxygenase, COX

Cat.No: T30529

Myelin Basic Protein (1-11)

Cat.No: T81734

Cat.No: TP2080

Cat.No: T69066

Cat.No: T63206

MOG (35-55), human

Cat.No: T39110

MOG peptide (35-55)

Cat.No: T78031

Cat.No: T82020

Synonym: Myelin basic protein (85-99) antagonist

ASP-4058 hydrochloride

Cat.No: T63141

Cat.No: T82621

Target: NOD-like Receptor (NLR)

6(5H)-Phenanthridinone

Cat.No: T72017

PDMP (hydrochloride)

Cat.No: T36015

γ-Fibrinogen 377-395 TFA

Cat.No: T80682

γ-Fibrinogen 377-395

Cat.No: T80683

MOG (92–106), mouse, rat

Cat.No: T81772

Cat.No: T69600

BIO5192 hydrate

Cat.No: T36296

[Leu144, Arg147]-PLP (139-151) TFA

Cat.No: T83690

Synonym: [Leu144, Arg147] Proteolipid Peptide (139-151),H-His-Ser-Leu-Gly-Lys-Leu-Leu-Gly-Arg-Pro-Asp-Lys-Phe-OH

Cat.No: T83688

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

Cat.No: T83910

Synonym: Sphingosine-1-Phosphate Lyase Inhibitor 31,S1PL Inhibitor 31,S1P Lyase Inhibitor 31

Cat.No: T38106

Cat. No.	Product Name	Target	Signaling Pathways
T3426	Bacoside A	MMP; Others; TNF; Dopamine Receptor; NOS; ROS	Apoptosis; GPCR/G Protein; Immunology/Inflammation; Neuroscience; Others; Proteases/Proteasome
	Bacoside A has a possible anticancer activity that could be inducing cell cycle arrest and apoptosis through Notch pathway in GBM in vitro. It exerts cytoprotective efficacy by attenuation of ROS generated through oxidative stress by an increase in the concentration of antioxidant enzymes and sustain membrane integrity which leads to restoring the damage caused by tBHP. Bacoside A can able to inhibit the progression of Experimental Autoimmune Encephalomyelitis (EAE) may be by the inhibition of i...
T36845	Isogarcinol
	Isogarcinol is a natural polyisoprenylated benzophenone first isolated from plant species in the genus Garcinia. It has immunosuppressant actions, inhibiting the protein phosphatase calcineurin (IC50 = 36 μM) and suppressing the proliferation of T cells. Oral administration of isogarcinol in mice decreases delayed type hypersensitivity, prolongs graft survival in allogeneic skin transplants, suppresses inflammation in collagen-induced arthritis, and reduces clinical symptoms in experimental auto...

天然产物

Cat.No: T3426

Target: MMP, Others, TNF, Dopamine Receptor, NOS, ROS

Cat.No: T36845

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