51
19
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T23101 |
o-3M3FBS
|
Others | Others |
o-3M3FBS 是 m-3M3FBS 的阴性对照。它以独立于 PLC 的机制及拮抗方式抑制内向和外向电流。它以与 m-3M3FBS 竞争的方式增加 [Ca2+]i 增加。 | |||
T3630 |
Relugolix
RVT-601,瑞卢戈利,TAK-385 |
GNRH Receptor | GPCR/G Protein |
Relugolix (RVT-601) 是口服有活性的非肽性促性腺激素释放激素的拮抗剂。同 TAK-013 相比,它对人和猴子的受体具有高亲和力和强拮抗活性,它们的 IC50值分别为0.33 nM 和0.32 nM。它可用于研究性激素依赖性疾病,如子宫肌瘤、子宫内膜异位症、前列腺癌等。 | |||
T67957 |
Pipoxizine
|
||
Pipoxizine 对组胺所致的支气管收缩具有拮抗作用,可用于研究哮喘疾病。 | |||
T0147 |
Clemastine fumarate
HS-592 (fumarate),富马酸氯马斯汀,Meclastine fumarate,Meclastine (fumarate) |
Autophagy; Histamine Receptor | Autophagy; GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Clemastine fumarate (Meclastine (fumarate)) 是一种合成乙醇胺,具有抗胆碱能、镇静和组胺 H1 拮抗作用。 | |||
T78646 |
Estrogen receptor antagonist 8
|
Estrogen Receptor/ERR | Endocrinology/Hormones |
Estrogen receptor antagonist8 作为一种雌激素受体ER的有效拮抗剂,在体内展现出抗子宫活性(EC50=4.160 μM)。 | |||
T67811 |
Tefludazine
|
||
Tefludazine 一种具有苯茚酮结构的新型神经抑制剂, 是一种具有良好口服活性且与多巴胺和5-羟色胺受体有拮抗作用的化合物。Tefludazine 在小鼠、大鼠和狗的体外和体内测试模型中表现出强大的多巴胺(DA)拮抗活性。Tefludazine 是一种用来治疗精神类疾病的潜在化合物。 | |||
T11851 |
Lin28-let-7a antagonist 1
|
Others | Others |
Lin28-let-7a antagonist 1 对 Lin28A-let-7a-1 相互作用的 IC50 为 4.03 μM,对 Lin28-let-7a 相互作用有明显的拮抗作用。 | |||
T2623 |
PD98059
PD 98059 |
ERK; Aryl Hydrocarbon Receptor; MEK; Autophagy | Autophagy; Immunology/Inflammation; MAPK |
PD98059 是一种 MEK 抑制剂,抑制 MEK1 和 MEK2 (IC50=2/50 μM),具有非 ATP 竞争性。PD98059 也是一种 AHR 的配体而起拮抗作用。PD98059 可以抑制细胞自噬。 | |||
T23380 |
Sonepiprazole
|
Dopamine Receptor | GPCR/G Protein; Neuroscience |
Sonepiprazole 是D4多巴胺受体选择性拮抗剂,与rD4多巴胺受体,hD4.2多巴胺受体,rD2多巴胺受体和组胺H1受体结合的Ki 分别为 3.6、10.1、5147 和 7430 nM。 | |||
T9833 |
Opiranserin hydrochloride
|
P2X Receptor; GlyT; 5-HT Receptor | GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience |
Opiranserin hydrochloride 是甘氨酸转运蛋白 2 型 (GlyT2) 和 5-羟色胺受体 2A (5HT2A) 的双重拮抗剂,IC50 分别为 0.86 和 1.3 μM。它显示对 rP2X3 的拮抗活性 (IC50=0.87 μM)。它正在开发为用于治疗术后疼痛的注射剂。 | |||
T23283 |
2-Methoxyidazoxan monohydrochloride
RX 821002 hydrochloride |
Adrenergic Receptor | GPCR/G Protein; Neuroscience |
L-Albizziin (2-Methoxyidazoxan monohydrochloride) 是高效的 alpha 2r 肾上腺素受体选择性拮抗剂,对 imidazoline 拮抗作用很小或没有。它对 (豚鼠) alpha 2D 肾上腺素受体 (pKd9.7) 的亲和力明显高于 (兔子) alpha 2A 肾上腺素受体 (pKd8.2)。 | |||
T31195 |
Dalcotidine
KU 1257,KU-1257 |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Dalcotidine (KU 1257) 是一种新型组胺H2受体拮抗剂,具有组胺H9受体拮抗活性和抗分泌作用,与豚鼠大脑皮层结合的Ki 值为0.040 对分离性豚鼠右心房组胺诱导的正变时反应的拮抗作用的KB 值为0.041。Dalcotidine 提高了溃疡愈合的质量,可能有助于降低溃疡的复发率和复发率。 | |||
T67894 |
Butyzamide
|
Thrombopoietin Receptor; JAK | Angiogenesis; Chromatin/Epigenetic; Immunology/Inflammation; JAK/STAT signaling; Stem Cells |
Butyzamide 是一种有效的 可口服的Mpl 激活剂,是一种对血小板生成素(TPO)受体具有拮抗作用的新型非肽基分子,促进表达人Mpl (hMpl)的和小鼠pro B 细胞株Ba/F3的增殖,诱导JAK2、STAT3、STAT5和MAPK 的磷酸化。Butyzamide 在小鼠异种移植试验中有助于提升血小板水平。 | |||
T9524 |
Lanthanum trichloride
|
Others | Others |
Lanthanum trichloride 可用作分析试剂,可用作提取金属镧的原料和石油裂化催化剂。它在医药领域也有一定的作用。例如,研究表明,它对内毒素(LPS)体内作用的拮抗作用对寻找新的有效内毒素拮抗剂有一定的影响,为防治内毒素血症提供了实验依据。 | |||
T67959 |
Pirodomast
|
Thrombin; Serine Protease | Proteases/Proteasome |
Pirodomast 是血栓素 A(TXA2)合成酶抑制剂。Pirodomast 能抑制白三烯(LT)D4、C4、E4 的形成和血栓素 B2(TXB2)的活性,但对组胺、甲氧胆碱、血清素、LTC4 或血小板活化因子诱导的豚鼠支气管痉挛的拮抗作用较弱或无效。Pirodomast 在体外对豚鼠气管只有微弱的松弛活性。Pirodomast 是一种潜在的抗过敏化合物,在体外可抑制胰蛋白酶的蛋白水解活性,在体内可阻止抗原诱发过敏绵羊的即时和晚期哮喘反应,抑制抗原诱导的过敏绵羊对组胺和卡巴胆碱的气道高反应性。 | |||
T23580 |
20681-S
20681 S |
||
20681-S has narcotic antagonistic properties and antinociceptive. | |||
T71159 |
F-0401
|
||
F-0401 is a novel calcium antagonist with platelet-activating factor-antagonistic action. | |||
T68838 |
Medroxalol hydrochloride
|
||
Medroxalol hydrochloride is an antihypertensive agent that possesses both alpha and beta-adrenergic antagonistic properties. | |||
T68690 |
Temiverine hydrochloride monohydrate
|
||
Temiverine hydrochloride monohydrate is an anticholinergic drug with calcium antagonistic activity. | |||
T68871 |
Pipradimadol
|
||
Pipradimadol is a 4,4-disubstituted piperidine derivative with antidepressive and serotonin antagonistic activity. | |||
T70634 | Psycholeine | ||
Psycholeine is isolated from the tropical plant Psychotria oleoides; exhibits somatostatin antagonistic activity on growth hormone secretion. | |||
T69021 | Nifedipine HCl | ||
Nifedipine HCl is a potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure. | |||
T36597 |
ISPA-28
|
||
ISPA-28 is a specific antagonist of the plasmodial surface anion channel (PSAC). It exerts its antagonistic effects by direct and reversible binding to CLAG3[1][2]. | |||
T38139 |
Orexin receptor antagonist 2
|
||
Orexin Receptor Antagonist 2 (compound 30), characterized by its potent antagonistic activity with pKis of 7.69 and 9.78, holds promise for insomnia research[1]. | |||
T28795 |
SKI2496
SKI 2496,SKI-2496 |
||
SKI2496 is a potent and orally bioavailableantagonist of Gonadotropin-Releasing Hormone Receptor (hGnRHR IC50 = 0.46 nM; max. LH inh. inh. (%, h)= 84%, 12h; LH inh. (24h) = 76%.). SKI2496 exhibits more selective antagonistic activity toward the human GnRH | |||
T71029 |
RCC-36 HCl
|
||
Rcc 36 is an active metabolite of temiverine that has inhibitory actions toward the atropine-resistant part of contractions, which may be related to the calcium antagonistic actions of these compounds. | |||
T80183 |
Muscarinic toxin 7
|
||
Muscarinic toxin 7,一种肽类毒素,特异性地针对毒蕈碱M1受体表现出选择性和非竞争性的拮抗活性。 | |||
T25911 |
Oxycinchophen
Magnophenyl,Sintofene,Reumartril,Chinoxone |
||
Oxycinchophen 是一种喹啉类的有机物,抗风湿病的化合物。它已被用于研究 P- 选择素拮抗活性,DHOD 抑制活性,以及抗炎药对血管平滑肌的作用。 | |||
T78013 |
Pep2-8 TFA
|
||
Pep2-8是增强PCSK9拮抗活性的肽,作用于前蛋白转化酶枯草杆菌蛋白酶/可辛9型(PCSK9)。 | |||
T71466 |
Sdz 210-096
|
||
Sdz 210-096 is a novel opiate antagonist. It is a novel 14 beta-benzyl morphinan derivative with antagonistic actions at mu and kappa opiate receptors. This compound has been characterized for luteinizing hormone (LH) secretion-stimulating effects in a variety of experimental paradigms in the rat. | |||
TP1075 |
AUNP-12 TFA (1353563-85-5 free base)
AUNP-12 TFA,NP-12 TFA |
||
AUNP-12 TFA (NP-12 TFA) is a polypeptide antagonist in the pd-1 signaling pathway, which has the same antagonistic effect on pd-l1 and pd-l2, and can protect the proliferation and effector function of lymphocytes. | |||
T78778 |
D3R/MOR antagonist 1
|
Dopamine Receptor | GPCR/G Protein; Neuroscience |
D3R/MOR antagonist 1 (Compound 114) 为D3R/MOR拮抗剂,其对D3R和MOR的Ki值分别为46.5 nM和691 nM。该化合物通过MOR的部分激动作用可能具有镇痛效果,同时通过D3R的拮抗作用有助于降低阿片类药物的滥用风险。 | |||
T79266 |
Antihypertensive agent 2
|
||
Antihypertensive agent 2 (Compound 4g) 为一种有效的血管紧张素 II 受体 1 拮抗剂,其降血压效能可与Losartan媲美或更胜一筹。 | |||
T83487 |
[Pmp1,Tyr(OEt)2] AVP
|
||
[Pmp1,Tyr(OEt)2] AVP为环状加压素(AVP)的线性拮抗剂,具备相似结构。 | |||
T82901 |
Belrestotug
GSK4428859A,EOS884448,EOS-448 |
||
Belrestotug (EOS-448) 是一种抗TIGIT (VSIG9, VSTM3) 的拮抗性人免疫球蛋白 G1 kappa (hIgG1 kappa) 抗体,具备抗肿瘤活性。 | |||
T61145 | Topiramate lithium | ||
Topiramate lithium (McN 4853) is a wide-ranging antiepileptic compound with GluR5 receptor antagonistic properties. Its mechanism of action involves enhancing GABAergic activity, inhibiting kainate/AMPA receptors, voltage-sensitive sodium and calcium channels, and increasing potassium conductance. Additionally, this compound inhibits carbonic anhydrase. [1][2][3] | |||
T61347 | D4R antagonist-1 | ||
D4R antagonist-1 是一种有效的选择性 D4R 拮抗剂,IC50为 6.87 μM。D4R antagonist-1 具有帕金森病研究潜力。 | |||
T75834 |
Antagonist G TFA
|
||
Antagonist G TFA 作为后叶加压素(vasopressin)的有效拮抗剂,同时对GRP和缓激肽具有弱拮抗作用。此外,Antagonist G 能够诱导AG-1转录,增强癌细胞对化疗的敏感性。 | |||
T26751 |
BBR 2160
BBR-2160,BBR2160 |
||
BBR 2160 is a dihydropyridine derivative belonging to the group of the so-called tiampidine. BBR 2160 has calcium-antagonistic properties in cardiac tissue. Intracellular microelectrodes have been used to characterize the electrophysiological properties o | |||
T80561 |
Atrosab
|
||
Atrosab是一种人源化IgG1抗TNFR1抗体,具有拮抗作用。它能够抑制TNF诱导的细胞凋亡(apoptosis),并减少IL-6和IL-8的生成,有助于研究炎症性疾病。 | |||
T73132 | DS69910557 | ||
DS69910557为高效、选择性的hPTHR1拮抗剂,口服有效。其对PTHR1的拮抗IC50值为0.08 μM。适用于甲状旁腺功能亢进症、恶性肿瘤引起的高钙血症及骨质疏松症研究。 | |||
T16399 | Opiranserin | P2X Receptor; GlyT; 5-HT Receptor | GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience |
Opiranserin 是一种非阿片类和非 NSAID 镇痛候选药物,是 2 型甘氨酸转运蛋白 (GlyT2) 和 5-羟色胺受体 2A (5HT2A) 的双重拮抗剂,IC50分别为 0.86 和 1.3 μM。它可用于术后疼痛的研究,对 rP2X3 有拮抗作用,IC50为0.87 μM。 | |||
T62918 |
GPR84 antagonist 3
|
||
GPR84antagonist 3 (compound 42)为一种高效GPR84(G 蛋白偶联受体 84)拮抗剂,具pIC50值为8.28,表现出对GTPγS的抑制作用,并拥有良好的药代动力学特性。 | |||
T60249 | RhlR antagonist 1 | ||
RhlR antagonist 1 is a highly effective antagonist of the RhlR protein, showing an IC50 value of 26 μM. It exhibits selective antagonistic activity against RhlR, with minimal effect on LasR and PqsR. RhlR antagonist 1 strongly inhibits biofilm formation in both static and dynamic environments and reduces the production of virulence factors, such as rhamnolipid and pyocyanin, in P. aeruginosa. These characteristics make RhlR antagonist 1 a valuable tool for the development of molecules that modul... | |||
T72492 | GnRH-R antagonist 1 | GNRH Receptor | GPCR/G Protein |
GnRH-R antagonist 1 (化合物 21a) 是GnRH-R拮抗剂,具有优良口服安全性及膜透性,高亲和力结合GnRH-R(IC50=0.57 nM),并展现出有效体外拮抗活性(IC50=2.18 nM)。该化合物适用于晚期前列腺癌治疗和预防过早LH峰出现的研究。 | |||
T80787 |
WAY-649123
|
||
WAY-649123为一有活性分子,适用于生化反应研究。 | |||
T79547 |
MOR agonist-2
|
Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
MOR agonist-2 (Compound 46) 为D3R拮抗剂及MOR激动剂,其Ki值分别为7.26 nM和564 nM。MOR agonist-2潜在以MOR部分激动机制实现镇痛效果,并通过D3R拮抗降低阿片类药物的滥用风险。 | |||
T74415 | Imlunestrant tosylate | ||
Imlunestrant (LY-3484356) tosylate 是口服有效且选择性的雌激素受体(estrogen receptor, ER)降解剂(SERD),具纯拮抗性。该化合物能持续抑制ER依赖的基因转录与细胞生长,适用于研究ER阳性(ER+)晚期乳腺癌(aBC)与子宫内膜样癌(EEC)。 | |||
T78734 |
Sigma-1 receptor antagonist 5
|
Sigma receptor | GPCR/G Protein |
Sigma-1 receptor antagonist 5 (compound 12) 是一种 4-吡啶衍生物,既有镇痛活性也是 sigma 受体 (Ki=4.5 nM (σ1R),10 nM (σ2R)) 及组胺 H3 (hH3R,Ki=7.7 nM,IC50=215 nM) 的拮抗剂。它能够抑制辣椒素引起的痛觉,并展现出对伤害性和神经性疼痛模型的显著疗效。 | |||
T70309 | Dicetrorelix pamoate | ||
Dicetrorelix pamoate is a synthetic decapeptide with gonadotropin-releasing hormone (GnRH) antagonistic activity. GnRH induces the production and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH) from the gonadotrophic cells of the anterior pituitary. Due to a positive estradiol (E2) feedback at midcycle, GnRH liberation is enhanced resulting in an LH-surge. This LH-surge induces the ovulation of the dominant follicle, resumption of oocyte meiosis and subsequently lutein... |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2S0271 |
Voacamine
老刺木胺,Voacanginine |
Cannabinoid Receptor; P-gp | GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience |
Voacamine (Voacanginine) 是非洲马铃果中的一种吲哚生物碱,可抑制多药耐药肿瘤细胞中的 P-糖蛋白作用,具有强效的大麻素 CB1受体拮抗活性。 | |||
T4S1659 |
Xanthotoxol
8-Hydroxypsoralen,8-Hydroxyfuranocoumarin,Psoralen,花椒毒酚,8-Hydroxypsoralene |
Reactive Oxygen Species; 5-HT Receptor; Endogenous Metabolite | GPCR/G Protein; Immunology/Inflammation; Metabolism; Neuroscience; NF-κB |
Xanthotoxol (Psoralen) 是一种具有生物活性的线性呋喃香豆素,具有很强的抗炎、抗氧化、5-HT 拮抗和神经保护作用等药理活性。 | |||
T20939 |
Bimatoprost acid
17-phenyl trinor PGF2α,17-phenyl trinor Prostaglandin F2α |
GPR | Endocrinology/Hormones; GPCR/G Protein |
Bimatoprost acid (17-phenyl trinor PGF2α) 是一种代谢稳定的 PGF2α 类似物,对 FP 受体具有潜在的拮抗活性。与 PGF2α 相比,它与绵羊黄体细胞上的 FP 受体结合的相对效力为 756%。 | |||
T6S1885 |
Benzoylmesaconine
Mesaconine 14-benzoate,苯甲酰新乌头原碱 |
Others | Others |
Benzoylmesaconine (Mesaconine 14-benzoate) 是乌头汤最丰富的组分。其中乌头汤可用于研究类风湿性关节炎。 | |||
T6S0659 |
Rhynchophylline
钩藤碱,Rhynchophyllin,Rhyncophylline,Mitrinermine,Mitrinermin |
Calcium Channel; NF-κB | Membrane transporter/Ion channel; Metabolism; NF-κB |
Rhynchophylline (Mitrinermine) 是一种生物碱类化合物,从钩藤中分离得到,具有很高的生物活性,被广泛用于抗炎、神经保护等方面的研究。 | |||
T15248 |
Estetrol
Donesta |
Estrogen Receptor/ERR; Endogenous Metabolite | Endocrinology/Hormones; Metabolism |
Estetrol(Donesta) 是可口服且具有选择性核雌激素受体 (estrogen receptor) 调节剂,是一种在怀孕期间由人类胎儿肝脏合成的天然雌激素。Estetrol 对子宫内膜或中枢神经系统有作用,但对乳房有拮抗作用。Estetrol 在低浓度时可能有助于降低血栓形成。Estetrol 可用于缓解更年期症状。 | |||
T6491 |
(-)-(S)-Equol
(−)-Equol,Equol,4',7-Dihydroxyisoflavan,4',7-Isoflavandiol,雌马酚 |
Estrogen Receptor/ERR; Estrogen/progestogen Receptor; Endogenous Metabolite | Endocrinology/Hormones; Metabolism |
(-)-(S)-Equol (4',7-Dihydroxyisoflavan) 是雌激素受体β的高亲和力配体。 | |||
T3915 |
Ginsenoside Ro
人参皂苷Ro,Chikusetsusaponin 5,Polysciasaponin P3,人参皂苷 Ro,Chikusetsusaponin V |
Calcium Channel; Reductase; Prostaglandin Receptor | Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism |
Ginsenoside Ro (Chikusetsusaponin V) 能降低 TXA2产量,较弱降低 COX-1 和 TXAS 活性,具有 Ca2+拮抗剂的抗血小板作用,IC50为 155 μM。 | |||
TN1719 |
Gymnestrogenin
匙羹藤苷元,(3BETA,4ALPHA,16BETA,21BETA)-齐墩果-12-烯-3,16,21,23,28-五醇 |
Liver X Receptor | Metabolism |
Gymnestrogenin has a dual LXRα±/α2 antagonistic profile. | |||
TN4821 |
Pregomisin
|
PAFR | GPCR/G Protein |
Pregomisin shows platelet-activating factor (PAF) antagonistic activity and the IC 50 value is 4.8x10(-5) M. | |||
TN6500 |
Microgrewiapine A
|
||
Microgrewiapine A is a selective cytotoxic agent for colon cancer cells over normal colon cells and to exhibit nicotinic receptor antagonistic activity for both the hα3β4 and hα4β2 receptor subtypes. | |||
TN6682 | Cyclo(Phe-Gly) | ||
Cyclo(Phe-Gly) shows weak antagonistic activity against VEGFR2 -CD, it also shows strong inhibitory activity against human cancer cells(KB,KBv200) with LD50 at 6.5 and 11.2 umol/L,respectively. | |||
T3P2855 | Chamigrenal | EGFR; NOS; PAFR; COX; Prostaglandin Receptor | Angiogenesis; GPCR/G Protein; Immunology/Inflammation; JAK/STAT signaling; Neuroscience; Tyrosine Kinase/Adaptors |
β-Chamigrenal has anti-inflammatory activity, it has inhibitory effects on lipopolysaccharide-induced nitric oxide and prostaglandin E2 production in RAW 264.7 macrophages. Chamigrenal shows platelet-activating factor antagonistic activity and the IC(50) | |||
TN2763 |
2-Hydroxy-3-methoxybenzoic acid glucose ester
|
PAFR | GPCR/G Protein |
2-Hydroxy-3-methoxybenzoic acid glucose ester shows a potent antagonistic activity against platelet activating factor (PAF), it can prevent the mice from the PAF-induced death at a dose of 300 micrograms/mouse. | |||
TN6678 |
Cyclo(Tyr-Pro)
|
||
Cyclo(Tyr-Pro) shows antibacterial activity towards several marine bacterial species, it also shows weak antagonistic activity against VEGFR2 -CD. Cyclo(Tyr-Pro) and cyclo(Pro-Val) are toxic to both suspension cells and seedlings of Pinus thunbergii, whic | |||
TN1815 | Kadsulignan L | HBV; PAFR | GPCR/G Protein; Microbiology/Virology |
Kadsulignan L shows in vitro antiviral effects on hepatitis B virus. It also shows moderate platelet-activating factor (PAF) antagonistic activities with the IC50 value of 2.6 x 10(-5) M. | |||
TN4319 |
Isopimaric acid
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Antifection | Microbiology/Virology |
Isopimaric acid is active against MDR and MRSA strains of S. aureus which are becoming increasingly resistant to antibiotics, the minimum inhibitory concentrations (MIC) are 32-64 microg/mL . Isopimaric acid is also possible that an antagonistic interacti | |||
TN4624 | Nantenine | Others | Others |
Nantenine is an acetylcholinesterase inhibitor, it functions as an effective antagonist against a wide range of MDMA-induced effects in mice. Nantenine has anticonvulsant effect, which seems attributable to its stimulation and the resultant decrease of Ca | |||
T35779 |
Oosporein
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Oosporein is a mycotoxin that has been found inBeauveriaand has diverse biological activities.1,2It is cytotoxic to Sf9 and Sf21 insect cells with 50% cytotoxic concentration (CC50) values of 4.23 and 10.43 μM, respectively.3Oosporin induces lethality in day-old cockerels (LD50= 6.12 mg/kg).4It inhibits Na+/K+-, Ca2+-, and Mg2+-ATPase activities by 27, 52, and 100%, respectively, in equine erythrocyte ghosts when used at a concentration of 200 μg/ml.2Oosporein inhibits herpes simplex 1 (HSV-1), ... |