Estradiol-d5 is deuterium labeled Estradiol. Estradiol is a steroid sex hormone vital to the maintenance of fertility and secondary sexual characteristics in females. Estradiol upregulates IL-6 expression through the estrogen receptor β (ERβ) pathway[1][2][3].
Conophylline is a vinca alkaloid extracted from leaves of a tropical plant Ervatamia microphylla. Conophylline is a differentiation inducer of for pancreatic cells. Conophylline suppresses HSC and induces apoptosis[1][2].
Pasireotide(SOM 230) is a stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9 respectively).IC50 value: 8.2/9.0/9.1/<7.0/9.9(pKi, sst1/2/3/4/5) [1]in vitro: SOM230 showed a lower potency of GH release inhibition (IC(50), 0.5 nM), compared with OCT (IC(50), 0.02 nM) and SRIF-14 (IC(50), 0.02 nM). A positive correlation was found between sst(2) but not sst(5) mRNA levels in the adenoma cells and the inhibitory potency of OCT on GH release in vivo and in vitro, and the effects of SOM230 and SRIF-14 in vitro [2]. In cultures of human fetal pituitary cells, SOM230 inhibited GH secretion by 42 +/- 9% (P = 0.002) but had no effect on TSH release. SOM230 inhibited GH release from GH-secreting adenoma cultures by 34 +/- 8% (P = 0.002), PRL by 35 +/- 4% from PRL-secreting adenomas (P = 0.01), and alpha-subunit secretion from nonfunctioning pituitary adenomas by 46 +/- 18% (P = 0.34) [3].in vivo: On day 7, there was a decrease in serum insulin levels from 1.06 ± 0.28 μg/L to 0.37 ± 0.17 μg/L (P = .0128) and a significant increase in serum glucose from 4.2 ± 0.45 mmol/L to 7.12 ± 1.06 mmol/L (P = .0075) in the treatment group but no change in the control group [4]. In wild-type mice, both octreotide and pasireotide significantly attenuated knee joint swelling and histopathologic manifestations of arthritis to an extent comparable to that of dexamethasone. In SSTR2(-/-) mice, the antiinflammatory effects of both octreotide and pasireotide were completely abrogated [5].
LGD-2226 is a selective and orally active androgen receptor modulator with an EC50 of 0.2 nM and a Ki of 1.5 nM for human androgen receptor. LGD-2226 shows tissue selectivity in animal models, with reduced effects on prostate compared to muscle. LGD-2226 can be used for muscle wasting, osteoporosis and sexual dysfunction[1][2].
FR-167653 is a selective p38 MAPK inhibitor.
Genistein 7,4'-di-O-β-D-glucoside is a natural product with significantly estrogenic proliferative effect in MCF-7 cells[1].
(D-Phe12,Nle21,38,α-Me-Leu37)-CRF (12-41) (human, rat) is a CRF antagonist. (D-Phe12,Nle21,38,α-Me-Leu37)-CRF (12-41) (human, rat) prevents the IL-1a induced Luteinizing hormone (LH) inhibition[1].
Oxprenoate potassium is a potent mineralocorticoid (MR) antagonist. Oxprenoate potassium accentuates DEX (dexamethasone)-induced apoptosis[1].
EP3 antagonist 3 (compound 2) is an orally active, potent and selective EP3 antagonist, with a pKi of 8.3. EP3 antagonist 3 shows excellent pharmacokinetic properties. EP3 antagonist 3 can be used for overactive bladder (OAB) research[1].
Thio-ITP (6-Thioinosine 5′-triphosphate) is a RNA polymerase activities competitive inhibitor[1].
L-Fucitol (1-Deoxy-D-galactitol) is a sugar alcohol isolated from Nutmeg[1].
INT-777 is a potent TGR5 agonist with an EC50 of 0.82 μM.
[Asp5]-Oxytocin is the first 5-position neurohypophyseal hormone analogue possessing significant biological activity[1].
Lodenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor for the treatment of erectile dysfunction (ED), with less oral bioavailability than Lodenafil carbonate[1].
Olmesartan medoxomil-d6 (CS 866-d6) is the deuterium labeled Olmesartan medoxomil. Olmesartan medoxomil is a potent and selective angiotensin AT1 receptor inhibitor with IC50 of 66.2 μM[1][2].
Norethindrone acetate is a female progestin approved by FDA for the treatment of endometriosis, uterine bleeding caused by abnormal hormone levels, and secondary amenorrhea.
Demoxytocin, a heterodetic cyclic peptide, is an analog of oxytocin. Demoxytocin affects the permeability of the cell membrane, increasing the content of calcium ions in smooth muscle cells, increasing its contraction. Demoxytocin also stimulates the contraction of smooth muscles of the uterus. Demoxytocin has the function of oxytocin. Demoxytocin can be used to research stimulation of labor in cases of premature rupture[1].
λ-Cyhalothrin is a high efficiency, broad-spectrum type II synthetic pyrethroid insecticide containing α-cyano group. λ-Cyhalothrin is used to control a wide range of pests in a variety of applications. λ-Cyhalothrin is a neurotoxin that targets sodium channels in the membranes of neurons in the central nervous system[1].
Pseudolaric acid A-O-β-D-glucopyranoside, isolated from Cortex Pseudolaricis, demonstrates antifungal and antifertility activities[1].
Pedalitin is a inhibitor of tyrosinase（IC50=0.28 mM） and α-glucosidase（IC50=0.29 mM）[1].
Bisphenol A-d16 is the deuterium labeled Bisphenol A[1]. Bisphenol A is a phenolic, organic synthetic compound widely used in the production of polycarbonate plastics and epoxy resins. Bisphenol A is a reproductive, developmental, and systemic toxicant, often classified as an endocrine-disrupting compound (EDC). Bisphenol A is associated with many diseases, including cardiovascular diseases, respiratory diseases, diabetes, kidney diseases, obesity, and reproductivedisorders[2][3].
A-123189 is a selective and potent α1D antagonist with Kis of 0.312 and 0.17 for human α1D and rat α1D, respectively. A-123189 displays selectivities between 10- to 20-fold for the α1D receptor over the human α1A and rat α1A receptors[1].
[Tyr1]-Somatostatin-14 could binds to SSTR2[1].
FR-167653 is a selective p38 MAPK inhibitor.
Indoramin is an orally active antihypertensive agent. Indoramin is also selective for the α1A-adrenoceptor[1].
Benoxathian hydrochloride is a potent α1 adrenoceptor antagonist, can be used for researching anorexia[1].
Alloisolithocholic acid (AILCA) activates large-conductance calcium-activated potassium (BK) channels with an EC50 value of 44.21 μM in Xenopus oocytes[1].
BHD is an effective, orally active and reversible contraceptive agent. BHD induces the apoptosis of spermatogenic cells rapidly and disruptes the blood-testis barrier effectively[1].
ADRA1D receptor agonist 1 (compound (R)-9S) is a potent, selective and orally active α1D adrenoceptor antagonist, with a Ki of 1.6 nM[1].
Human Growth Hormone (1-43) is an N-terminal fragment of human growth hormone with specific and pronounced insulin-like activity. Human Growth Hormone (1-43) can be used to study the function and metabolic pathways of growth hormone, a potential obesity-related factor[1].