(R)-Pirtobrutinib ((R)-LOXO-305) is a less active enantiomer of Pirtobrutinib. Pirtobrutinib (LOXO-305), a highly selective and non-covalent next generation BTK inhibitor, inhibits diverse BTK C481 substitution mutations[1].
Inflachromene (ICM) is a microglial inhibitor with anti-inflammatory effects, directly binds high mobility group protein 1 (HMGB1) and HMGB2 and reduces their cytoplasmic accumulation in microglial cells; blocks the sequential processes of cytoplasmic localization and extracellular release of HMGBs by perturbing its post-translational modification; effectively downregulates proinflammatory functions of HMGB and reduces neuronal damage in vivo.
1-Pyrenebutyric acid is a fluorescence probe that can be used in fluorescence determination of DNA. 1-Pyrenebutyric acid can be used as a linker for biomolecules to form a self-assembled monolayer on grapheme[1].
(S)-2-(Benzylamino)-3-(4-hydroxyphenyl)propanoic acid is a tyrosine derivative[1].
MB05032 is a special and efficacious GNG inhibitor targeted the AMP binding site of fructose 1,6-bisphosphatase (FBPase) with an IC50 value of 16 nM. IC50 Value: 16 nM (Human Liver FBPase) [1]Target: Fructose 1, 6-bisphosphataseOral delivery of MB05032 was achieved by using the bisamidate prodrug MB06322 (CS-917), which is converted to MB05032 in two steps through the action of an esterase and a phosphoramidase.in vitro: MB05032 inhibits human liver FBPase with a potency (IC50 = 16 ± 1.5 nM) significantly greater than the natural inhibitor, AMP (IC50 = 1 μM), and the most well characterized AMP mimetic, ZMP (IC50 = 12 ± 1.4 μM). MB05032 inhibits rat FBPase 3-fold weaker (IC50 of 61 ± 4 nM) than human FBPase, whereas AMP is 20-fold weaker as an inhibitor [1]. Inhibition of FBPase activity in islet β-cells by its specific inhibitor MB05032 led to significant increase of their glucose utilization and cellular ATP to ADP ratios and consequently enhanced GSIS in vitro [2]. in vivo: Oral administration of MB06322 to young (8-9 weeks old) ZDF rats with mild diabetes (basal insulin levels of 7.7 ± 0.7 ng/ml) and aged (12-13 weeks) ZDF rats with overt diabetes (basal insulin levels of 0.65 ± 0.16 ng/ml) results in dose-dependent glucose lowering. The dose-response is relatively steep, with 6-10 mg/kg and 30-100 mg/kg being the approximate doses associated with minimal and maximal activity, respectively [1]. Pretreatment of mice with the MB05032 prodrug MB06322 could potentiate GSIS in vivo and improve their glucose tolerance [2].Toxicity: Neither lactate nor triglycerides increased in 8- to 9-week-old ZDF rats with mild diabetes treated with high doses of MB06322. In ZDF rats with more advanced disease, lactate and triglyceride levels were elevated but only modestly (<2-fold). These results suggest that, unlike inhibitors of other GNG enzymes, FBPase inhibitors may lower glucose with an adequate safety margin [1].Clinical trial: Evaluation of Glucose Lowering Effect, Safety and Tolerability of CS-917. Phase 2b
(R)-mchm5U is a diastereomer of (S)-mchm5U (HY-153100A)[1].
H-Gly-Arg-Ala-Asp-Ser-Pro-OH (GRADSP) is a negative control peptide of GRGDdSP[1].
RAD140 is a potent, orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM). IC50 value: 7 nM (Ki, fot androgen receptor) [1]Target: androgen receptor in vitro: RAD140 demonstrates excellent affinity for the androgen receptor (Ki = 7 nM) as well as good selectivity over other steroid hormone nuclear receptors, with the closest off target receptor being the progesterone receptor (IC50 = 750 nM). [1] RAD140 is a novel SARM with high affinity and specificity for AR, is orally available, and exhibits potent anabolic effects in rodents and nonhuman primates.[2]in vivo: The stability of RAD140 is high (t1/2 > 2 h) in incubations with rat, monkey, and human microsomes, and it also had good bioavailability in rats and monkeys. [1] RAD140 is also neuroprotective using the rat kainate lesion model. RAD140 is shown to exhibit peripheral tissue-specific androgen action that largely spared prostate, neural efficacy by activation of androgenic gene regulation effects, and neuroprotection of hippocampal neurons against cell death caused by systemic administration of the excitotoxin kainate.[2]
2-(((Benzyloxy)carbonyl)amino)propanoic acid is an alanine derivative[1].
Sorbitol dehydrogenase-IN-1 is a potent and orally active sorbitol dehydrogenase inhibitor with IC50 s of 4, 5 nM for rat and human, respectively[1].
Acanthopanaxoside B is a triterpenoid saponin isolated from the leaves of Acanthopanax senticosus[1].
Maximin 7 is an antimicrobial peptide derived from toad Bombina maxima[1].
6-Azidohexanoyl-Val-Cit-PAB is a click chemistry reagent that can be used to synthesis vaccine[1].
1-Hydroxymethyl-β-carboline glucoside (Compound 13) is a natural product that can be isolated from Picrasma quassioides[1].
Plecstatin-1 is a potent organoruthenium anti-cancer agent[1]. Plecstatin-1 selectively targets plectin (a scaffold protein and cytolinker) in tumour spheroids[1].
PYBG acts as a versatile precursor to be facilely conjugated with various fluorescent dyes through ‘Click chemistry’ and Sonogashira coupling reactions[1].
Caprooyl-tetrapeptide-9 (AcTP1) is a bioactive peptide with anti-aging effect and has been reported used as a cosmetic ingredient[1].
Physion 8-O-β-D-glucoside is a bioactive component of Fallopia multiflora, can be used for the research of dizziness[1].
Chebulic acid, a phenolcarboxylic acid compound isolated from Terminalia chebula, has potent anti-oxidant activity, which breaks the cross-links of proteins induced by advanced glycation end-products (AGEs) and inhibits the formation of AGEs. Chebulic acid is effective in controlling elevated metabolic parameters, oxidative stress and renal damage, supporting its beneficial effect in diabetic nephropathy[1][2].
2-(tert-Butylamino)acetic acid hydrochloride is a Glycine (HY-Y0966) derivative[1].
DiFMUP is a fluorogenic substrate, and has been widely used for the continuous detection of phosphatase activities. DiFMUP is hydrolysis by a phosphatase results in the release of Xuorescent DIFMU, which can be easily followed in continuous mode by a Xuorescence reader[1][2].
Dehydrosoyasaponin I methyl ester (Soyasaponin Be methyl ester) is a saponin found in Trifolium alexandrinum[1].
IHRIC is a penta-peptide, correlated positively with hairpin DNA with tetramer loops. Therefore, IHRIC joins hands with hairpin DNA (hpDNA) with improved selectivity as sensing materials in the detection system, used for surface plasmon resonance imaging (SPRi)[1].
EtDO-P4 is a nanomolar inhibitor of glycosphingolipid (GSL) synthesis. EtDO-P4 suppresses activation of the EGFR-induced ERK pathway and various receptor tyrosine kinases (RTKs). EtDO-P4 can be used for various types of cancer, including Burkitt’s lymphoma[1].
BigLEN(rat), one of the most abundant peptides in brain, is a potent GPR171 agonist, with an EC50 of 1.6 nM[1][2].
Quercetin 3,3'-dimethyl ether possesses antioxidant acticity[1].
Aszonalenin is a metabolite of Aspergillus zonatus[1].
Boc-3-Pal-OH is an alanine derivative[1].
Notum pectinacetylesterase-1 is a potent inhibitor of notum pectinacetylesterase. Notum pectinacetylesterase-1 can be used for the research of disorders affecting the bone[1].
MAGE-3 (271-279) is a 271-279 residue peptide derived from melanoma antigens encoded by MAGE-3. MAGE-3 is a cytolytic T lymphocyte (CTL)-defined MAGE-3 protein associated with the human leukocyte antigen (HLA)-A2 molecule. MAGE-3 is overexpressed in different human tumor types, including malignant melanoma, but not by normal tissues except for testis and placenta[1].